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Protein Tyrosine Kinase
PI3K/Akt/mTOR

MAPK
Cytoskeletal
Signaling

Apoptosis

120,000 +Inhibitors

Cell Cycle

Epigenetics
Ubiquitin
SignalingDNA
Damage

Stem
Cells

阻害剤
Selleckは120,000種類以上のシ

グナル伝達経路研究に使用される阻害剤を供給しています。

Others
Neuronal Signaling

HTS化合物ライブラリー
Bioactive Compound Library-Ⅰ
4560 compounds

Bioactive Compound Library-Ⅱ (Provided by Pfizer)
2863 compounds

FDA-approved Drug Library1890 compounds

Kinase Inhibitor Library
599 inhibitors

Natural Product Library

Target Selective Inhibitor Library

1605 natural products

641 validated bioactive compounds

Express-Pick Library (Provided by Pfizer)

Epigenetics Compound Library

4208 chemical compounds

265 small molecule modulators

Clinical Compound Library

Stem Cell Signaling Compound Library

603 clinical compounds

102 small molecule inhibitors

Metabolism Compound Library

Inhibitor Library

492 chemical compounds

2134 inhibitors

Immunology/Inflammation Compound Library...

400 chemical compounds

目的の化合物を選択してライブラリーのカスタマイズが出来ます。

2013年1月から現在まで、Selleck製品を使用して、Nature、Science、

Cellで発表された学術論文は158件にも及びます。

SelleckはPfizer社が開発した化合物のライセンスサプライヤーです

Nature, 2018, 559(7713):211-216

Nature, 2016, 537(7620):422-426

Cell, 2018, 174(6):1477-1491

Nature, 2018, 560(7718):372-376

Nature, 2016, 530(7590):358-61

Cell, 2018, 174(5):1200-1215

Nature, 2018, 560(7716):112-116

Nature, 2016, 534(7607):341-6

Cell, 2018, 174(5):1127-1142

Nature, 2018, 559(7713):285-289

Nature, 2016, 32(7597):107-11

Cell, 2018, 175(1):186-199

Nature, 2018, 560(7718):387-391

Nature, 2016, 531(7596):651-5

Cell, 2018, 174(2):338-349

Nature, 2018, 561(7724):551-555

Nature, 2015, 528(7582):422-6

Cell, 2018, 174(2):406-421

Nature, 2018, 560(7718):325-330

Nature, 2015, 522(7557):492-6

Cell, 2018, 174(2):422-432

Nature, 2018, 560(7716):117-121

Nature, 2015, 527(7576):100-4

Cell, 2018, 174(2):391-405

Nature, 2018, 560(7719):499-503

Nature, 2015, 522(7556):349-53

Cell, 2018, 175(1):85-100

Nature, 2018, 558(7708):141-145

Nature, 2015, 521(7552):316-21

Cell, 2018, 175(2):429-441

Nature, 2018, 559(7713):279-284

Nature, 2015, 521(7553):541-4

Cell, 2018, 174(4):953-967

Nature, 2018, 555(7694):103-106

Nature, 2015, 520(7549):683-7

Cell, 2018, 174(5):1216-1228

Nature, 2018, 554(7692):317-322

Nature, 2015, 518(7538):254-7

Cell, 2018, 174(4):856-869

Nature, 2018, 555(7698):673-677

Nature, 2015, 517(7534):391-5

Cell, 2018, 175(2):442-457

Nature, 2018, 555(7696):387-391

Nature, 2015, 522(7555):226-30

Cell, 2018, 173(1):104-116

Nature, 2018, 556(7702):501-504

Nature, 2015, 517(7535):460-5

Cell, 2018, 173(1):117-129

Nature, 2018, 557(7704):247-251

Nature, 2015, 523(7558):92-5

Cell, 2018, 173(4):972-988

Nature, 2018, 557(7704):256-260

Nature, 2015, 521(7552):357-61

Cell, 2018, 173(6):1413-1425

Nature, 2018, 553(7686):101-105

Nature, 2015, 520(7547):368-72

Cell, 2018, 173(2):470-484

Nature, 2018, 553(7686):96-100

Nature, 2015, 524(7566):471-5

Cell, 2018, 172(4):857-868

Nature, 2018, 553(7686):91-95

Nature, 2015, 517(7536):583-8

Cell, 2018, 173(2):515-528

Nature, 2017, 545(7652):54-59

Nature, 2015, 519(7543):370-3

Cell, 2018, 172(4):841-856

Nature, 2017, 547(7664):453-457

Nature, 2014, 511(7507):90-3

Cell, 2018, 172(3):564-577

Nature, 2017, 549(7673):548-552

Nature, 2014, 510(7504):283-7

Cell, 2018, 172(3):439-453

Nature, 2017, 549(7673):533-537

Nature, 2014, 509(7498):105-9

Cell, 2018, 172(1-2):90-105

Nature, 2017, 551(7679):247-250

Nature, 2014, 508(7494):118-22

Cell, 2018, 172(3):423-438

Nature, 2017, 550(7675):270-274

Nature, 2013, 501(7466):237-41

Cell, 2017, 171(7):1545-1558

Nature, 2017, 550(7676):402-406

Nature, 2013, 500(7461):222-6

Cell, 2017, 171(7):1611-1624

Nature, 2017, 552(7683):121-125

Nature, 2013, 498(7452):109-12

Cell, 2017, 171(5):1094-1109

Nature, 2017, 550(7677):534-538

Nature, 2013, 496(7446):523-7

Cell, 2017, 171(4):824-835.e18

Pfizer社の品質保証に則って製造された化合物もあります。すべての化合物はNMRとHPLCを使用して検Nature, 2017, 552(7683):116-120

Nature, 2013, 493(7430):51-5

Cell, 2017, 171(3):628-641

Nature, 2017, 551(7678):105-109

Science, 2018, 361(6405)

Cell, 2017, 161(4):803-16

品されています。

Nature, 2017, 551(7682):639-643

Science, 2018, 359(6378)

Cell, 2017, 171(1):217-228

Nature, 2017, 550(7674):133-136

Science, 2018, 11(528)

Cell, 2017, 171(3):668-682

Nature, 2017, 550(7676):360-365

Science, 2018, 11(525)

Cell, 2017, 170(5):860-874.e19

Nature, 2017, 548(7668):466-470

Science, 2018, 10(441)

Cell, 2017, 170(3):548-563.e16

Nature, 2017, 549(7672):404-408

Science, 2018, 10(436)Cell, 2017, 170(5):845-859.e19

Nature, 2017, 548(7669):582-587

Science, 2018, 10(433)

Cell, 2017, 170(3):507-521.e18

Nature, 2017, 548(7668):471-475

Science, 2018, 11(530)

Cell, 2017, 169(2):243-257.e25

Nature, 2017, 548(7667):343-346

Science, 2017, 9(420)Cell, 2017, 169(2):216-228.e19

Nature, 2017, 170(5):860-874.e19

Science, 2017, 3(11):e1701679

Cell, 2017, 168(5):856-866

Nature, 2017, 546(7658):431-435

Science, 2017, 9(414)10

Cell, 2017, 168(1-2):86-100

Nature, 2017, 546(7658):416-420

Science, 2017, 358(6367):eaan4368

Cell, 2016, 167(1):233-247

Nature, 2017, 545(7654):365-369

Science, 2017, eaal3755

Cell, 2016, 167(7):1803-1813

Nature, 2017, 543(7647):728-732

Science, 2017, 355(6320):78-83

Cell, 2016, 164(1-2):293-309

Nature, 2017, 541(7638):481-487

Science, 2017, 355(6320):84-88

Cell, 2016, 165(1):234-46

Nature, 2017, 542(7641):362-366

Science, 2016, 354(6315)

Cell, 2015, 162(2):441-51

Nature, 2016, 539(7627):54-58

Science, 2016, 351(6277):aad3680

Cell, 2015, 160(1-2):161-76

Nature, 2016, 540(7631):119-123

Science, 2016, 352(6283):353-8

Cell, 2014, 159(5):1110-25

Nature, 2016, 539(7629):437-442

Science, 2016, 352(6282):189-96

Cell, 2014, 158(5):989-99

Nature, 2016, 539(7628):304-308

Science, 2016, 353(6302):929-32

Cell, 2013, 154(5):1036-46

Nature, 2016, 538(7626):477-482

Science, 2013, 341(6146):651-4

Cell, 2013, 153(4):840-54

Nature, 2016, 535(7613):517-22

Science, 2013, 339(6120):700-4

2013年にSelleckはPfizer社とライセンス契約を結んだことで、Pfizer社の多様な化合物が提供可能となりました。これらの化合物は疾患研究において幅広い用途を有しています。

◆ 生物活性化合物はPfizer社のライセンスを得ており、臨床試験で安全かつ効果があることが実証されています。
◆ 取り扱う化合物は抗癌化合物（例：Bosutinib）から、抗生物質耐性研究で使用するグリシルサイクリン抗生物質（例：Tigecycline）まで、多岐にわたります。
◆ 信頼性保証：Pfizer社からライセンスを得た化合物はすべてPfizer社が開発し、検品しています。一部◆ 詳細な前臨床研究データと安全性情報を利用することが出来ます。

Table of Contents
PI3K/Akt/mTOR

Epigenetics

Methylation

Immunology & Inflammation

PI3K

1

mTOR

3

Akt

4

GSK-3

4

ATM/ATR5PDK

5

S6 Kinase

5

AMPK

6

DNA-PK

6

MELK

6

HDAC

7

PARP

8

JAK

9

Pim

10

HIF

10

Aurora Kinase

10

Sirtuin

11

DNA Methyltransferase

11

Histone Methyltransferase

11

Epigenetic Reader Domain

12

Histone Demethylase

13

Histone Acetyltransferase

13

DNA Methyltransferase

11

LSD1

14

JMJD

14

EZH1/2

14

G9a/GLP

14

PRMT

15

SETD

15

MLL

15

COMT

15

DOT1

16

HNMT

16

SMYD2

16

WDR5

16

SAM MTase

16

PPMTase16

Protein Tyrosine Kinase

Angiogenesis

PD-1/PD-L1

17

COX

18

CCR

19

Histamine Receptor

19

IL Receptor

20

gp120/CD4

20

CXCR

20

MALT

20

LTR

20

NOS

20

NADPH-oxidase

21

VEGFR

22

EGFR

23

PDGFR

25

c-Met

25

HER2

26

IGF-1R

26

FLT3

27

FGFR

27

c-Kit

28

Src

28

ALK

29

Tie-2

29

c-RET

29

TAM Receptor

29

CSF-1R

30

Ephrin Receptor

30

BTK

30

Trk Receptor

30

ACK

31

VEGFR

22

JAK

9

EGFR

23

PDGFR

25

HER2

26

FLT3

27

FGFR

27

HIF

10

VDA

33

Bcr-Abl

33

Src

28

ALK

29

Apoptosis

Autophagy

ER stress & UPR

JAK/STAT

MAPK

Cytoskeletal Signaling

Syk

33

Kinesin

46

FAK

34

Microtubule Associated

46

BTK

30

Integrin

47

PAK

47

Dynamin

47

CDK

48

PD-1/PD-L1

17

Bcl-2

35

Caspase

36

p53

36

PD-1/PD-L1

17

TNF-alpha36

Aurora Kinase

10

Mdm2

36

Chk

49

Survivin

37

ROCK

50

c-RET

29

PLK

50

IAP

37

APC

50

PERK

37

Wee1

50

ASK

37

Rho

51

DYRK

51

c-Myc

51

TGF-beta/Smad52

Bcr-Abl

33

PKC

46

ROCK

50

HDAC

7

ATM/ATR

5

PARP

8

Sirtuin11

Topoisomerase

53

DNA-PK

6

Telomerase

54

MTH1

54

GSK-3

4

JAK

9

STAT

41

TGF-beta/Smad52

Wnt/beta-catenin

45

ROCK

50

Gamma-secretase

55

Hedgehog/Smoothened

56

Casein Kinase

56

Hippo Pathway

56

Autophagy

38

CXCR

20

LRRK2

39

JNK

40

HSP (e.g. HSP90)

40

PERK

37

ASK

37

JAK

9

STAT

41

EGFR

23

Pim

10

MEK

42

Raf

43

p38 MAPK

43

JNK

40

ERK

44

TOPK

44

MNK

44

Akt

4

Bcr-Abl33

Wnt/beta-catenin

45

PKC

46

FAK

34

HSP (e.g. HSP90)

40

Cell Cycle

TGF-beta/SmadDNA Damage

Stem Cells & Wnt

Ubiquitin

Neuronal Signaling

NF-κB

Metabolism

Proteasome

57

DUB

57

E3 Ligase

58

p97

58

E1 Activating

58

E2 Conjugating

58

Beta Amyloid

59

5-HT Receptor

59

COX

18

Gamma-secretase

55

GluR

60

Adrenergic Receptor

61

AChR

62

Histamine Receptor

19

Dopamine Receptor

63

Opioid Receptor

63

GABA Receptor

63

P-gp

64

P2 Receptor64

OX Receptor

64

BACE

64

Substance P

64

NMDAR

65

CaMK

65

GlyT

65

HDAC

7

NF-κB

66

IκB/IKK

66

NOD1

67

GPCR & G Protein

Liver X Receptor

72

FAAH

72

CETP

72

Lipase73

Transferase

73

Ferroptosis

73

Lipoxygenase73

HMG-CoA Reductase

73

AhR

74

Casein Kinase

56

NAMPT

74

IDO

74

Decarboxylase

74

GLUT

74

PKM

75

5-HT Receptor

59

Adrenergic Receptor

61

Histamine Receptor

19

Dopamine Receptor

63

Opioid Receptor

63

Cannabinoid Receptor

76

Endothelin Receptor

77

S1P Receptor

77

Hedgehog/Smoothened

56

SGLT

77

LPA Receptor

77

OX Receptor

64

PAFR

77

PKA

78

Adenosine Receptor

78

CaSR

78

CXCR

20

PPAR

68

Vasopressin Receptor

78

P450 (e.g. CYP17)

69

cAMP

78

HSP (e.g. HSP90)

40

PDE

69

Hydroxylase

70

5-alpha Reductase

79

Factor Xa

70

Estrogen/progestogen Receptor

79

DHFR

70

Androgen Receptor

80

Dehydrogenase

71

RAAS

80

Procollagen C Proteinase71

Opioid Receptor

63

Phospholipase (e.g. PLA)

71

Aromatase81

Carbonic Anhydrase

72

GPR

81

MAO

72

Endocrinology & Hormones

82

Sodium Channel

83

ATPase84

Potassium Channel

84

GABA Receptor

63

P-gp

64

Proton Pump

84

CFTR

85

TRPV

85

CRM1

85

Proteasome57

Caspase36

Gamma-secretase55

HCV Protease

86

DPP-4

87

HIV Protease

87

MMP

Microbiology

PI3K/Akt/mTOR
RTK

Rictor87

Tyrosinase

88

Cysteine Protease88

Glutaminase88

Pan-PI3K Inhibitors
BEZ235
GDC-0941
LY294002
Selective PI3K Inhibitors
HS-173 (p110α)
TGX-221 (p110β)
CZC24832 (p110γ)
CAL-101 (p110δ)

86

Integrase

89

Reverse Transcriptase

90

CCR

19

HIV Protease

87

C-Abl
PDK-1 Inhibitors
OSU-03012
BX-795
BX-912
PHT-427

Ca2+
PI3K

Akt

GBL

Wee1

Pan-Akt Inhibitors
MK-2206
Perifosine
GSK690693
Selective Akt Inhibitors
A-674563 (Akt1)
CCT128930 (Akt2)

Pan-mTOR Inhibitors
AZD8055
KU-0063794
PP242
Selective mTOR Inhibitors
Rapamycin (mTORC1)
Everolimus (mTORC1)

GSK-3

Raptor

Pan-GSK-3 Inhibitors
CHIR-99021
SB216763
CHIR-98014
Selective GSK-3 Inhibitors
TWS119 (GSK-3β)
Tideglusib (GSK-3β)

CaspaseeNOS

Cell Cycle

p53

p70S6K

DNA-PK Inhibitors
NU7441
NU7026
KU-0060648
PIK-75

S6

Apoptosis

Bcl-2
NO

NF-κB

Cyclin D1

FOXO3AS6 Kinase Inhibitors
BI-D1870
PF-4708671
AT7867

Bcl-2

Mdm2

DNA-PK

DEPTOR

PKC
mTOR

ROCK
HSP

mTOR

Syk

PI3K

PI3K

DEPTOR

BCR

Ras

PDK-1

Protein Synthesis

HCV Protease

Bcr-Abl Inhibitors
Imatinib
Ponatinib
Nilotinib
Bafetinib
Dasatinib

Cytokines

GBL

mTOR

87

Serine Protease

GPCR

PI3K

mTORC1

Proteases

Calcium Channel

mTORC2

Transmembrane Transporters

Bim
Pan-Bcl-2
Inhibitors
ABT-737
ABT-263
TW-37
Selective Bcl-2
Inhibitor
ABT-199 (Bcl-2)

Cardiovascular Homeostasis

Bax

PI3K
阻害選択性
Inhibitor Name

PI3K

p110α

p110β

p110δ

p110γ

Dactolisib (BEZ235)++++ IC50: 4 nM++

IC50: 75 nM+++ IC50: 7 nM++++ IC50: 5 nM

Pictilisib (GDC-0941)++++ IC50: 3 nM++

IC50: 33 nM++++ IC50: 3 nM++

LY294002+

IC50: 0.5 μM +Buparlisib (BKM120)++

IC50: 52 nM

PI-103++++ IC50: 2 nM

IC50: 0.97 μM +Idelalisib (CAL-101)

TGX-221

IC50: 166 nM++

IC50: 89 nM
IC50: 262 nM++++ IC50: 3 nM++++ IC50: 5 nM++

IC50: 0.1 μM+

IC50: 0.5 μM

Clinical Phase
Phase 2mTOR

Phase 2Phase 4
+ IC50: 2.4 μM

Phase 3

DNA-PK,mTOR+++ IC50: 15 nM

+

mTOR

IC50: 29 μM
DNA-PK,ATM,MLCK

IC50: 36 nM+++ IC50: 23 nM

Phase 2

IC50: 49 nM

Phase 1

IC50: 39 nM+

IC50: 383 nM++

IC50: 37 nM +++ IC50: 16 nM++

IC50: 44 nM++++ IC50: 4.6 nM+

IC50: 270 nM+

IC50: 300 nM +++ IC50: 8 nM+

IC50: 0.51 μM ++IC50: 76 nM+

IC50: 60 μM++++

Other Targets
mTOR (p70S6K),ATR

DNA-PK++++ IC50: 3 nM

XL147 analogue
ZSTK474

IC50: 75 nM

IC50: 116 nM +++++ IC50: 3 nM

IC-87114
Wortmannin

++

Vps34

IC50: 0.57 μM++++ IC50: 2.5 nM+

C2βAlpelisib (BYL719)++++ IC50: 5 nM

AS-605240++

PIK-75 HCl+++ IC50: 5.8 nM

IC50: 60 nM++

Phase 33-Methyladenine (3-MA)
A66++

IC50: 32 nM

Voxtalisib Analogue++

IC50: 39 nM++

IC50: 113 nM++

IC50: 43 nM

PIK-93++

IC50: 39 nM+

IC50: 590 nM++

IC50: 120 nM +++ IC50: 16 nM

DNA-PK+ IC50: 25 μM+ IC50: 462 nM+++ IC50: 9 nM

PI4Kβ
DNA-PK,mTOR

Phase 2

+ IC50: 140 nM + IC50: 320 nM PI4KIIIβ,DNA-PK,ATM

1

阻害選択性Inhibitor Name

阻害選択性
PI3K

p110α

p110β

p110δ

p110γ

++++ Ki: 0.024 nM++++ Ki: 0.06 nM

IC50: 58 nM+++ IC50: 18 nM

Omipalisib (GSK458)++++ Ki: 0.019 nM ++++ Ki: 0.13 nM

PIK-90+++ IC50: 11 nM+

PF-04691502++++ Ki: 1.8 nM++++ Ki: 2.1 nM

AZD6482+

Apitolisib (RG7422)++++ IC50: 5 nM

IC50: 27 nM+++ IC50: 7 nM+++ IC50: 14 nM

GSK1059615++++ IC50: 0.4 nM ++++ IC50: 0.6 nM++++ IC50: 2 nM++++ IC50: 5 nM++++ Ki: 1564 pM++++ Ki: 23 pM++

IC50: 870 nM +++ IC50: 10 nM

Duvelisib (IPI-145)
Gedatolisib (PKI-587)++++ IC50: 0.4 nM

TG100-115

+

++

+

BGT226 (NVP-BGT226)++++ IC50: 4 nM++++++ Ki: 1.6 nM++

IC50: 1.2 μM

+

++
++
+

PIK-294

IC50: 63 nM
IC50: 54 nM
IC50: 490 nM+++

Copanlisib (BAY 80-6946)++++ IC50: 0.5 nM ++++ IC50: 3.7 nM

IC50: 4.5 μM

YM201636+

CH5132799+++ IC50: 14 nM++++ IC50: 0.7 nM

IC50: 0.12 μM ++++++ IC50: 7 nM

IC50: 165 nM +IC50: 215 nM

VS-5584 (SB2343)++++ IC50: 2.6 nM +++ IC50: 21 nM

Taselisib (GDC 0032)++++ Ki: 0.29 nM+++ Ki: 9.1 nM+

CZC24832
Bimiralisib (PQR309)++++ Kd: 1.5 nM

Phase 2mTOR

Phase 1mTOR++

IC50: 38 nM

mTOR
HDAC1,HDAC3,HDAC10++++ Kd: 11 nM

Phase 2Phase 2

IC50: 160 nM
IC50: 0.25 μM+++ IC50: 6.4 nM

Phase 3+++ IC50: 14 nM+++ IC50: 24 nM

IC50: 10 μM+++ IC50: 16 nM++++++ IC50: 3.0 nM++++ Ki: 0.12 nM++++ Ki: 0.97 nM+++++ Kd: 25 nM

mTOR

IC50: 50 nM++++ IC50: 2.7 nM

mTOR+ IC50: 292 nM +IC50: 27 nM
mTOR

Phase 2Phase 2

IC50: 282 nM
sumoylation,Axl,IRAK4+++ IC50: 24.5 nM ++Phase 1
Phase 2

IC50: 374 nM+++ Kd: 25 nM+

Phase 4Phase 2

IC50: 33.2 nM++++ IC50: 2.5 nM

IPI-3063
Autophinib+++ IC50: 19 nM

IPI-549

Autophagy
Phase 1+++ IC50: 16 nM

Serabelisib (INK-1117)

Phase 2+++ IC50: 21 nM

SF2523++

GDC-0326

IC50: 34 nM++++ Ki: 0.2 nM+++

Ki: 26.6 nM++++ Ki: 4 nM

DNA-PK,BRD4,mTOR

IC50: 158 nM+++ Ki: 10.2 nM

SAR405++++ IC50: 1.2 nM+++ IC50: 22.2 nM

umbralisib (TGR-1202)

Phase 3

VPS34 inhibitor 1+++ IC50: 15 nM

GDC-0084++++ Ki: 2 nM

AZD8835+++ IC50: 6.2 nM +++Ki: 46 nM++++ Ki: 3 nM+++ Ki: 10 nM

IC50: 431 nM+++ IC50: 5.7 nM

++

mTOR

+

PIK-III

Phase 2Phase 1

IC50: 90 nM++++ pKi: 9.9

Nemiralisib (GSK2269557)

Phase 2

IC50: 1.2μM+++ IC50: 0.018μM

VPS34-IN1+++ IC50: 25 nM

Voxtalisib (XL765)++

IC50: 39 nM++

IC50: 113 nM++

IC50: 43 nM+++ IC50: 18 nM

AMG319AZD8186++

PF-4989216

IC50: 35 nM++++ IC50: 4 nM++

IC50: 36 nM++

IC50: 36 nM+

IC50: 1078 nM +++ IC50: 15 nM

Quercetin+

IC50: 5.4 μM

GSK2636771√

Pilaralisib (XL147)++

IC50: 39 nM

PI-3065
HS-173+

DNA-PK,mTOR

Phase 2Phase 2

IC50: 850 nM+++ IC50: 12 nM++++ IC50: 1 nM++++ IC50: 2 nM+++ IC50: 9 nM

Phase 1++

Inhibitor Name

PI3K

p110α

IC50: 65 nM
Phase 2

p110δ

p110γ

C2β

Vps34

Other Targets

Clinical Phase
Phase 1

√
√

mTOR
阻害選択性
Inhibitor Name

mTOR

mTORC1mTORC2Other Targets

Clinical Phase
Phase 2

Dactolisib (BEZ235, NVP-BEZ235)+++

Rapamycin (Sirolimus)++++ IC50: ~0.1 nM

Everolimus (RAD001)+++

AZD8055++++ IC50: 0.13 nM

Phase 1

Temsirolimus (CCI-779, NSC 683864)+

IC50: 1.76 μM

Phase 4

PI-103+

IC50: 30 nM

p110α,p110γ,p110δ

IC50: 6 nM

Phase 4Phase 4

IC50: 1.6 nM-2.4 nM

p110α,p110δ,p110β++

Torkinib (PP242)+++

Ridaforolimus (Deforolimus, MK-8669)++++ IC50: 0.2 nM

Sapanisertib (INK 128, MLN0128)++++ Ki: 1.4 nM

Voxtalisib (SAR245409, XL765) Analogue+

IC50: 157 nM

Torin 1+++

IC50: 4.32 nM

IC50: ~10 nM++

IC50: ~10 nM
p110δ,PDGFR,DNA-PK

IC50: 8 nM

Omipalisib (GSK2126458, GSK458)

Phase 3+++

IC50: 2 nM++

IC50: 10 nM

PI3Kα,PI3Kγ,PI3Kδ

Phase 2PI3Kγ,PI3Kα,PI3Kδ

Phase 2

DNA-PK,p110γ,C2α++++ Ki: 0.18 nM++++ Ki: 0.3 nM

p110α,p110δ,p110γ

Phase 1++

OSI-027+++

IC50: 4 nM

PI3Kγ

Phase 1

PF-04691502++

Ki: 16 nM

PI3Kδ,PI3Kα,PI3Kγ

Phase 2

Apitolisib (GDC-0980, RG7422)+

Ki app: 17 nM

p110α,p110δ,p110γ

Phase 2

GSK1059615++

IC50: 12 nM

PI3Kα,PI3Kβ,PI3Kδ

Phase 1

Gedatolisib (PF-05212384, PKI-587)++++ IC50: 1.6 nM

PI3Kα,PI3Kγ

Phase 2

WYE-354+++

IC50: 5 nM

Vistusertib (AZD2014)+++

IC50: 2.8 nM

P-Akt (S473),pS6 (S235/236)

Phase 2

Torin 2++++ IC50: 0.25 nM

WYE-125132 (WYE-132)++++ IC50: 0.19 nM

PP121

++

IC50: 13 nM

WYE-687+++

IC50: 7 nM

WAY-600++

IC50: 9 nM

ETP-46464++++ IC50: 0.6 nM

GDC-0349+++

Ki: 3.8 nM

XL388

++

IC50: 9.9 nM

SF2523+

IC50: 280 nM

CZ415

++

pIC50: 8.07

CC-223++

IC50: 16 nM

cFMS,FLT4,DNA-PK

Phase 2

Voxtalisib (XL765, SAR245409)+

IC50: 157 nM

PI3Kγ,PI3Kα,PI3Kδ

Phase 2

Zotarolimus(ABT-578)+++

IC50: 2.8 nM

Tacrolimus (FK506)√

BGT226 (NVP-BGT226)√

Palomid 529 (P529)+++ IC50: 23 nM

p110β

GSK2292767

KU-0063794
Phase 1

IC50: 36 nM

IC50: 35 nM

Tenalisib (RP6530)

IC50: 22 nM

IC50: 65 nM

ATM,ATR,DNA-PKPDGFR,Hck,VEGFRATR,DNA-PK,PI3Kα
PI3Kα
+++

IC50: 8 nM+

Phase 1

IC50: 166 nM
DNA-PK,PI3Kα,PI3Kγ

Phase 4Phase 4PI3Kα,PI3Kγ,PI3Kβ

Phase 2Phase 1√

LY3023414√

DNA-PK,class I PI3K isoforms

Chrysophanic Acid

√

EGFR

Phase 2++++ IC50: 0.8 nM

CAY10505+

IC50: 3.0 μM+

IC50: 2.4 μM

PKC,Src,Sirtuin

Phase 4Phase 2√

Deguelin√

Akt

LY3023414√

DNA-PK,mTOR kinase

2

Phase 2Phase 2

IC50: 83 nM
Casein Kinase 2

IC50: 0.24 μM ++++ IC50: 12 nM++

Phase 1mTOR

IC50: 33 nM

IC50: 0.50 μM ++IC50: 1.1 μM

Seletalisib (UCB-5857)
2-D08

DNA-PK

PIKfyve++

PIK-293

TG100713

Phase 2Phase 3

IC50: 3.3 μM++++ IC50: 2 nM

P-Akt,P-Akt,mTOR

Ki: 243 pM

IC50: 39 nM+++ IC50: 10 nM

Clinical Phase
Phase 1+++

AS-604850

PKI-402

IC50: 235 nM ++Other Targets
mTORC1,mTORC2

GNE-317++++ Ki: 1.9 nM

IC50: 80 nM

IC50: 935 nM+++ IC50: 19 nM

Vps34+++ IC50: 5.4 nM

IC50: 1.3 μM +AS-252424

CUDC-907

IC50: 350 nM

C2βPhase 2

3

Akt

ATM/ATR

阻害選択性

阻害選択性

Inhibitor Name

Akt

MK-2206 2HCl
Perifosine (KRX-0401)

Akt1
+++

Akt2

IC50: 8 nM

+++

Akt3

IC50: 12 nM+++++ IC50: 2 nM+++

IC50: 13 nM+++

IC50: 9 nM

Ipatasertib (GDC-0068)++++ IC50: 5 nM++

IC50: 18 nM+++

IC50: 8 nM

AZD5363++++ IC50: 3 nM+++

IC50: 8 nM+++

IC50: 8 nM++++ IC50: 3.8 nM

AT7867
Triciribine++

IC50: 32 nM

IC50: 17 nM++

IC50: 47 nM+++

A-674563+++

IC50: 6 nM

Ki: 11 nM

Ki: 2.7 μM+++++ IC50: 5 nM

Akti-1/2++

IC50: 58 nM

Uprosertib (GSK2141795)+

IC50: 180 nM

Afuresertib (GSK2110183)++++ Ki: 0.08 nM

AT13148++

IC50: 38 nM++++ IC50: 4.5 nM++

IC50: 16 nM+

IC50: 210 nM+

IC50: 2119 nM+

IC50: 328 nM++

IC50: 38 nM++++ Ki: 2 nM+++

IC50: 50 nM+++

Phase 1

KU-60019++++ IC50: 6.3 nM

Phase 2

VE-821ROCK2Phase 2

Wortmannin++

IC50: 150 nM

PI3Kδ,PI3Kα,PI3Kγ

Phase 2

Torin 2++

EC50: 28 nM

CP-466722+

IC50: 410 nM

PKCθ,PKCη,PrkX

PKA,p70 S6K
Phase 2

IC50: 19 nM
IC50: 14 nM

PKA,CDK2,GSK-3β

CGK 733++

IC50: 200 nM++

IC50: 200 nM

AZ20
Phase 2++++ IC50: <0.0062 μM

AZD1390++++ IC50: 0.78 nM

BAY 1895344 (BAY-1895344)+++

Phase 2

AZD6738++++ IC50: 1 nM

Phase 1

Schisandrin B (Sch B)+

Phase 4

AZD0156

ERK

Deguelin

√

PI3K

PDK

TIC10

√

ERK

阻害選択性

阻害選択性

IC50: 10 nM++++ IC50: 6.7 nM++

IC50: 34.3 nM++

CHIR-98014++++ IC50: 0.65 nM++

IC50: 30 nM+

IC50: 60 nM+

IC50: ~78 nM

BIO

+++
+

AZD1080

IC50: 10 nM

IC50: 6.9 nM

TDZD-8Phase 1

2-D08+++

IC50: 10 nM

Clinical Phase
Phase 1

BX-795++++ IC50: 6 nM

c-Kit,CDK2/CyclinE,Chk1

BX-912+++

IC50: 12 nM

PKA,KDR,CDK2/CyclinE

PHT-427+

Ki: 5.2 μM

Akt

GSK2334470+++

IC50: 10 nM

S6 Kinase
阻害選択性
Inhibitor Name

p70 S6K

p70 S6K1

RSK1
++

+

IC50: 31 nM

RSK2
++

IC50: 24 nM

PF-4708671+ IC50: 160 nM

Ki: 38 nM

H 89 2HCl+ IC50: 80 nM

IC50: 2 μM

LJH685+++ IC50: 6 nM+++

Phase 2

LJI308+++ IC50: 6 nM++++ IC50: 4 nM

Phase 4+++

IC50: 11 nM

LY2584702 Tosylate++++ IC50: 4 nM+++

IC50: 10 nM

LY2584702++++ IC50: 4 nM

AT13148+++

IC50: 53 nM

1-Azakenpaullone++

IC50: 18 nM

Indirubin+

IC50: 0.6 μM

sumoylation,Axl,IRAK4

IC50: 18 nM

IC50: 8 nM

RSK4Other Targets

Clinical Phase++ IC50: 15 nM
Akt2,PKA,Akt1

IC50: 31 nM++++ IC50: 0.9 nM

RSK3
++

IC50: 85 nM

++

++

4

Other Targets

IC50: 5 μM

++

IM-12

Bikinin

PDK1++

BI-D1870++++ IC50: 6.7 nM+++++ IC50: 1.5 nM

Phase 2
P-gp

IC50: 7.25 μM

OSU-03012 (AR-12)

AT7867+++

BIO-acetoxime

Phase 4

IC50: 68 nM

AR-A014418

LY2090314

Phase 3

TYK2,CDK5/p35,CDK2/CyclinA++++ IC50: 5 nM

CHIR-99021 (CT99021)
AZD2858

IC50: 78 nM

Phase 1

IC50: ~34.3 nM

Tideglusib+

Clinical Phase++++ IC50: 0.58 nM

TWS119SB415286

Other Targets

mTOR

√

Inhibitor Name

GSK-3

mTOR,DNA-PK,PI3Kα

IC50: 7 nM

PKA,ROCK2,ROCK1√

Phase 2Phase 1

Phase 2√Clinical Phase

mTOR,DNA-PK++++ IC50: 5 nM

AZ32

SC66

Other Targets
p110α,p110γ,mTOR (p70S6K)

PI3K,DNA-PK,MLCK+++

TIC10 Analogue+++

EC50: 35 nM

+++

MEK

SB216763++

IC50: 545 nM

PI3K,PKC

CHIR-99021 (CT99021) HCl

Ki: 13 nM+√

GSK-3β++ETP-46464√

GSK-3αIC50: 21 nM

p70 S6K,PKA

Honokiol

GSK-3

+++
IC50: 12.9 nM

VE-822

Miltefosine

Inhibitor Name

ATR

KU-55933 (ATM Kinase Inhibitor)++++ Ki: 2.6 nM

IC50: 402 nM

ATM

Phase 3

PDK1

Miransertib (ARQ 092) HCl

Inhibitor Name
Dactolisib (BEZ235, NVP-BEZ235)

HIV-1

CCT128930

PHT-427++

IC50: 130 nM+

Clinical Phase
Phase 2

IC50: 4.7 μM+

GSK690693

PF-04691502

Other Targets

IC50: 65 nM

PKA
IC50: 5 nM++++ IC50: 4 nM+++

IC50: 13 nM
Phase 1
Phase 1+

IC50: 85 nM

PKA,ROCK2,ROCK1

Phase 1

CDK2/CyclinA,CDK5/p35,CDK1/CyclinB√5

Epigenetics

AMPK
阻害選択性
Inhibitor Name

AMPK

Dorsomorphin (Compound C) 2HCl++

WZ4003++++ IC50: 20 nM

Dorsomorphin (Compound C)++

Ki: 109 nM

HTH-01-015+++

IC50: 100 nM

Ki: 109 nM

Epigenetic “Reader”

Epigenetic “Writer”

DNA-PK

Alteration of
DNA-templated Process

Addition of Chemical
Modification

DNA Methyltransferase
Inhibitors
Decitabine
Azacitidine
SGI-1027
RG108
Zebularine

Pan Inhibitors
I-BET151
I-BET-762
UNC669Selective Inhibitors
PFI-1 (BRD4)
RVX-208 (BD2)
UNC1215 (L3MBTL3)

Epigenetic “Eraser”
Removal of
Modification

Recruitment

阻害選択性
Inhibitor Name

DNA-PK

Other Targets

PI-103++

IC50: 23 nM

NU7441 (KU-57788)+++

IC50: 14 nM

PIK-75 HCl++++ IC50: 2 nM

NU7026+

IC50: 0.23 μM

PI3K

PP121

+

IC50: 60 nM

PDGFR,Hck,VEGFR

KU-0060648++++ IC50: 5 nM

PI3Kδ,PI3Kβ,PI3Kα

SF2523+++

IC50: 9 nM

PI3Kα,PI3Kγ,BRD4

LTURM34++

IC50: 0.034 μM

CC-115+++

IC50: 0.013 μM

LY3023414√

DNA Methylation

Clinical Phase

p110α,p110δ,p110β

Histone Acetylation
Histone Acetyltransferase
Inhibitors
C646
MG149

Histone Methylation

mTOR,PI3Kα

Phase 2mTOR kinase,class I PI3K isoforms

Phase 2

Histone Methyltransferase
Inhibitors
EPZ5676
EPZ005687
BIX 01294
MM-1023-deazaneplanocin A

Histone Phosphorylation

阻害選択性
Inhibitor NameOTSSP167

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Not clear - only putative targets so far:
- MBD2- TET enzymes leading to iterative
oxydation resulting in eventual removalof methyl-cytosine

Histone Acetyltransferases (HATs)
GCNS/PCAF
GNAT Related (e.g., HAT1, TFIIIC)
Myst Family (e.g., TIP60, HBO1)
CBP/p300 Family
TAF250 Family
Src Family (e.g., SRC1, TIF2)

Bromodomain Proteinse.g.,most HATs
BET Family (Brd2, Brd, Bdf1)
Brg-1

Histone Deacetylases (HDACs)Class I (HDAC1, HDAC2, HDAC3, HDAC8)Class IIa (HDAC4, HDAC5, HDAC7, HDAC9)Class IIb (HDAC6, HDAC10)
Sirtuins (SIRT1-SIRT7)Class IV (HDAC11)

Lysine methyltransferases (KMTs)
KMT1A - KMT1F (e.g., G9a, GLP)MLL Family (e.g., NSD1)
DOT1
KMT3A - KMT3C (e.g., NSD1)
DOT1
KMT5A, KMT5B (e.g., SUV420H1)
KMT6/ EZH2
KMT7/ SET7&9
KMT8/ RIZ1Royal Family- Chromo-domain Proteins,
e.g., HP-1 like, polycomb like,
CHD like- Tudor-domain Proteins,
e.g., SMN
- PHD Proteins,
e.g., CBD, ING2, DNMT3L, PHF6

Lysine Demethylases (KDMs)
LSD1/ KDM1
JHDM/Jumonji (e.g., JHDM1A/B,
JHDM2A/B, JHDM3A-D,
JARID1A-D, UTX)

Serine/Threonine Kinases
e.g.,MST, AMPK
Haspin, VRK, Aurora B
PKCα, PKCβ, MSK1/2, JNK

14-3-3 Proteins
Seven Isoforms: theta, gamma, zeta, eta,
epsilon, beta, mu

Protein Phosphatasese.g.,Serine/Threonine Protein Phosphatases(PPP2CA, PPP2CB, PPP1CC),
Protein Phosphatase 1D,
Eye-absent Homologues (EYA1-3)

DNMT3B

p110α,p110γ,p110δ

MELK

MeCP2
MBD1-4

DNMT1
DNMT3A

MELK+++

IC50: 0.41 nM

HDAC
阻害選択性
Inhibitor Name

HDAC

Vorinostat (SAHA)+++
IC50: ~10 nM

HDAC2

Panobinostat++++
IC50: 5 nM

Trichostatin A (TSA)++++
IC50: ~1.8 nM

HDAC3

HDAC4

HDAC5

HDAC6

HDAC7

HDAC8

HDAC9

HDAC10

Other
Targets

Clinical Phase

Phase 3Phase 3Phase 1+
IC50: 0.59 μM

Phase 2Phase 2+++
IC50: 36 nM+++
IC50: 47 nM

Phase 3++
IC50: 100 nM

MC1568+++
IC50: 15 nM

Tubastatin A HCl+
IC50: 854 nM++++
IC50: 7.5 nM

Givinostat (ITF2357)

6

HD2

+++
IC50: 27 nM

Romidepsin (FK228)

Dacinostat (LAQ824)+++
IC50: 32 nM

CUDC-101++++
IC50: 4.4 nM

++++
+++
++++
+++
+++
IC50: 4.5 nM IC50: 12.6 nM IC50: 9.1 nM IC50: 13.2 nM IC50: 11.4 nM

Quisinostat 2HCl

++++
++++
++++
++++
++++
IC50: 0.11 nM IC50: 0.33 nM IC50: 4.86 nM IC50: 0.64 nM IC50: 3.69 nM

Pracinostat (SB939)++
IC50: 49 nM

PCI-34051

HD1+
IC50: 1.7 μM++++
IC50: 0.15 μM IC50: 0.29 μM IC50: 1.66 μM

Mocetinostat

HDAC11

Phase 3+
IC50: 0.51 μM

Entinostat (MS-275)

Belinostat (PXD101)

HDAC1

++
IC50: 96 nM+++
IC50: 43 nM++
IC50: 56 nM++++
IC50: 5.1 nM

+
++
++
+++
IC50: 373 nM IC50: 79.8 nM IC50: 67.2 nM IC50: 26.1 nM++++
IC50: 4.26 nM

+++
+
++
++
IC50: 47 nM IC50: 1.008 μM IC50: 137 nM IC50: 140 nM++
IC50: 70 nM+++
IC50: 10 nM

Phase 3

EGFR,HER2

Phase 1++++++++
IC50: 0.46 nM IC50: 0.37 nM

Phase 2+++
IC50: 40 nM

Phase 3++
IC50: 93 nM+++
IC50: 10 nM

7阻害選択性Inhibitor Name

阻害選択性

HDAC

HDAC1

HDAC2

Droxinostat++++
Ki: 7 nM

Abexinostat+++
Ki: 19 nM

HDAC5

HDAC7

HDAC8

+
IC50: 2.47 μM+
IC50: 1.46 μM++++
Ki: 8.2 nM+++
Ki: 17 nM+
IC50: 280 nM

HDAC9

HDAC10

HDAC11

HD1

HD2

Other
Targets

Clinical Phase

Ricolinostat++
IC50: 51 nM

Tacedinaline (CI994)+
IC50: 0.9 μM+
IC50: 0.9 μM+
IC50: 1.2 μM

CUDC-907++++
IC50: 1.7 nM++++
IC50: 5.0 nM++++
IC50: 1.8 nM++++
IC50: 4.7 nM+++
IC50: 24 nM

Phase 3++
IC50: 100 nM++++
IC50: 2.8 nM

RG2833 (RGFP109)

Resminostat+++
IC50: 42.5 nM++
IC50: 50.1 nM

PI3Kα,PI3Kδ,PI3Kβ+++

IC50: 2.1 nM

IC50: 8.0 μM++

IC50: 0.3 μM

Phase 1

ME0328+

IC50: 6.3 μM

Phase 2

Pamiparib (BGB-290)++++ IC50: 0.83 nM

NMS-P118++

Valproic acid+
IC50: 0.4 mM++
IC50: 160 nM+++
IC50: 45 nM++
Ki: 60 nM+++
IC50: 46 nM

BG45+
IC50: 2 μM

4SC-202+++
IC50: 1.20 μM IC50: 1.12 μM IC50: 0.57 μM+
IC50: 2.2 μM+++
Ki: 26 nM

Phase 3+++
Ki: 15 nM++++
IC50: 2.6 nM++
IC50: 137 nM+++
IC50: 36 nM++
IC50: 120 nM

Phase 1+
IC50: 11.3 μM+
IC50: 50 μM+
IC50: 21 μM+
IC50: 9.7 μM

Phase 2++++
IC50: 2 pM+++
IC50: 11.9 nM

LMK-235++++
IC50: 4.2 nM+
IC50: 60 μM++++
IC50: 119 pM++++
IC50: 5 nM

Nexturastat A++
IC50: 157 nM

TMP269HPOB+
IC50: 4.4 μM++
IC50: 97 nM+
IC50: 1.7 μM+++
IC50: 43 nM++
IC50: 56 nM+++
IC50: 23 nM+
IC50: 2.8 μM+
IC50: 3.0 μM

Valproic acid sodium salt√

GABA receptor,
Autophagy

Phase 4

Curcumin√Nrf2,NF-κB,p300 histone
acetylatransferase

Phase 4

Scriptaid√

Sodium Phenylbutyrate

Phase 4√

Tasquinimod(-)-Parthenolide+

IC50: 400 nM+++

Phase 3√
p53,MDM2 ubiquitination,
NF-κB

√

PARP
阻害選択性
Inhibitor Name

Phase 2

IC50: 3.8 nM+++

IC50: 2.1 nM

Phase 3√Phase 1

BGP-15 2HCl√

Phase 2

PARP

PARP1

阻害選択性

PARP2

PARP3

Clinical Phase

Ruxolitinib (INCB018424)

JAK1
+++

IC50: 3.3 nM

JAK2

++

AZD1480++++ IC50: 0.26 nM

Fedratinib (SAR302503, TG101348)+++

AT9283++++ IC50: 1.2 nM+

Tofacitinib (CP-690550,Tasocitinib)+

IC50: 112 nM++

IC50: 20 nM++++ IC50: 1 nM

WP1066+

IC50: 2.3 μM

TG101209+++

IC50: 6 nM+

IC50: 169 nM++

IC50: 48.0 nM++

IC50: 44 nM++++ IC50: ~0.5 nM++

IC50: 18.68 nM+++

IC50: 10.76 nM

Baricitinib (LY3009104, INCB028050)+++

IC50: 5.9 nM

+++

++

IC50: 53 nM++

IC50: 50 nM++++ IC50: 1.8 nM
++

XL019

+

IC50: 134.3 nM++++ IC50: 2.2 nM

S-Ruxolitinib (INCB018424)+++

IC50: 3.3 nM++++ IC50: 2.8 nM

ZM 39923 HCl+

pIC50: 4.4+

IC50: 520 nM+

IC50: 1.8 μM+

IC50: 214.2 nM

pIC50: 7.1

PF-06651600++

IC50: 33.1 nM

FM-381++++ IC50: 127 pM
IC50: 10nM++

IC50: 18nM+

IC50: 11 nM+++

Ki: 13 nM++++ Ki: 2.5 nM

Cerdulatinib (PRT062070, PRT2070)+++

IC50: 12 nM+++

IC50: 6 nM+++

IC50: 8 nM++++ IC50: 0.5 nM

Filgotinib (GLPG0634)+++

IC50: 10 nM++

IC50: 28 nM+

IC50: 810 nM+

IC50: 116 nM

FLLL32+

IC50: <5 μM

BMS-911543++++ IC50: 1.1 nM+

IC50: 75 nM++

IC50: 66 nM

Phase 3

Go6976√

Curcumol√Phase 1
Phase 3Phase 3+++√Phase 3

TGM2,EGFR+++

GLPG0634 analogue

FLT3 (D835Y),FLT3

PDGFRβ,FLT3

Decernotinib (VX-509)

Phase 3Phase 2Phase 3

IC50: 19 nM

Oclacitinib maleate

IC50: 99nM

FLT3,FLT4,FGFR2

EGFR,Src,VEGFR

++
+

√

IC50: <50 nM

IC50: 19 nM

WHI-P154

Peficitinib (ASP015K, JNJ-54781532)++

IC50: 5.7 nM

Phase 1

RET,FLT3++++ IC50: 3 nM

Itacitinib (INCB39110)

Ki: <5 nM

STAT3

IC50: 31.63 nM

Pacritinib (SB1518)

Phase 2Phase 4

IC50: 19.8 nM

CEP-33779

Phase 3

Aurora A,Aurora B,Abl1 (T315I)

Phase 2++++++ IC50: <3 nM

FLT3,RET

IC50: 155 nM++

Phase 3++

IC50: 1 nM-10 nM

NVP-BSK805 2HCl+++

AG-14361+++

Gandotinib (LY2784544)

Ki: 5.2 nM++++ IC50: 0.57 nM++++ IC50: 1.1 nM

IC50: 18 nM++

Talazoparib (BMN 673)

Phase 4

IC50: 3 nM

AZ 960

Clinical Phase

Phase 1++

Veliparib (ABT-888)
Ki: 1.4 nM

Other Targets

Phase 4

IC50: 11 nM

Phase 4+++

Tyk2++++ IC50: 1 nM+++++++ IC50: 1 nM

Rucaparib (AG-014699,PF-01367338) phosphate

IC50: 20 nM

Momelotinib (CYT387)

IC50: 5 nM

Ki: 2.9 nM

JAK3++++ IC50: 2.8 nM

Tofacitinib (CP-690550) Citrate++8++++ IC50: 1.2 nM

AZD2461

Olaparib (AZD2281, Ku-0059436)

INO-1001 (3-Aminobenzamide)

Phase 3√

Inhibitor Name+
IC50: 289 nM

CAY10603+
IC50: 2.9 μM

IC50: 3.3 μM++++ IC50: 0.11 nM

JAK++
IC50: 78 nM

BRD73954

Santacruzamate A+

Iniparib (BSI-201)++
IC50: 67 nM

TMP195

Citarinostat

Benzamide

IC50: 0.89 μM

Phase 4++
Ki: 59 nM+++
IC50: 35 nM

IC50: 95 μM+++++
IC50: 0.4 nM

ACY-738

Tucidinostat+

Phase 3Phase 2++++
IC50: 1.7 nM++
IC50: 95 nM

Clinical Phase

Kd: 0.009 μM++++ IC50: 1 nM

Picolinamide

Niraparib (MK-4827) tosylate+++
IC50: 15 nM+++++++
IC50: 8.35 nM IC50: 15.4 nM

PARP3

EC50: 20 nM
IC50: 3.8 nM

Phase 2++
IC50: 71.8 nM

Ki: 1.5 nM+

NU1025

Tubastatin A

WT161

++

PJ34 HCl

E7449

++++
IC50: 5.4 nM

PARP2
+++

+++

++++
IC50: 4 nM++
Ki: 5 nM

PARP1++++ Ki: 1 nM

UPF 1069++
IC50: 100 nM++
Ki: 32 nM

PARP

Niraparib (MK-4827)

Phase 3+++
IC50: 27 nM

Tubacin

Inhibitor Name
A-966492+++
IC50: 30 nM++
IC50: 48 nM

Splitomicin

HDAC6

+
IC50: 16.9 μM++
IC50: 58 nM

M344

HDAC4

++
IC50: 80 nM

RGFP966

AR-42

HDAC3

+

IC50: 84nM+++

Ki: 13 nM

Phase 3
ARK5,MST1,Fms

Phase 2Phase 3

SET-2

Phase 2Phase 3√Phase 2Phase 2
FLT3,PKCα,PKCβ1
Phase 3Phase 2

9

Pim

阻害選択性

阻害選択性

Inhibitor Name

Inhibitor Name

Pim1

Pim2

Pim3

SGI-1776 free base++

IC50: 7 nM

SMI-4a++IC50: 17 nM

PIM447 (LGH447)++++ Ki: 6 pM

CX-6258 HCl+++

IC50: 5 nM+

IC50: 25 nM++

IC50: 16 nM

AZD1208+++

IC50: 0.4 nM+++

IC50: 5 nM+++

IC50: 1.9 nM

IC50: 363 nM+

Clinical Phase

FLT3

Phase 1

IC50: 69 nM+++++ Ki: 18 pM

Other Targets

Phase 1++++ Ki: 9 pM

Phase 1

阻害選択性
Inhibitor Name

HIF

HIF1

PHD1

PHD2

IOX2

+++
++

Molidustat (BAY 85-3934)++

Roxadustat (FG-4592)√

2-Methoxyestradiol (2-MeOE2)√

Chetomin√

IC50: 20 μM+

IC50: 480 nM++

IC50: 3.9 μM+++

IC50: 280 nM

Phase 2+++Phase 3

IC50: 450 nM

Other Targets+

IC50: 350 nM

SNS-314 Mesylate+++

IC50: 9 nM++

IC50: 31 nM

BI-847325++

IC50: 25 nM++++ IC50: 3 nM++

IC50: 15 nM

MEK2,MEK1

Reversine+++

IC50: 12 nM+++

IC50: 13 nM++

IC50: 20 nM

human A3 adenosine receptor

Clinical Phase

FLT3,RET,VEGFR3/FLT4

Phase 2++++ IC50: 3 nM

Sirtuin

PX-478 2HCl√

Phase 3
Microtubule AssociatedPhase 2Phase 3sGC
Phase 1DMOG

Inhibitor Name

SIRT1

Selisistat (EX 527)++++ IC50: 38 nM

Sirtinol+

IC50: 131 μM

OSS_128167+

IC50: 1578 μM

3-TYP++++ IC50: 88 nM

SIRT2

SIRT3

Sirtuin

SIRT6

Other Targets

Clinical Phase
Phase 2++

IC50: 38 μM++

IC50: 89 μM++

IC50: 89 μM++++ IC50: 16 nM
Phase 4++++ IC50: 28 nM

SirReal2
AGK2
Tenovin-6

√
√

+++
++

IC50: 3.5 μM

IC50: 21 μM++

Nicotinamide (Vitamin B3)Salermide

p53

IC50: 67 μM

Phase 4√√

DNA Methyltransferase
阻害選択性√Phase 1√

Aurora Kinase
阻害選択性
Inhibitor Name

Aurora A

Alisertib (MLN8237)++++ IC50: 1.2 nM

Tozasertib (VX-680, MK-0457)++++ Ki app: 0.6 nM

Aurora B

Aurora C

Other Targets++

Ki app: 18 nM

ZM 447439+

IC50: 110 nM+

IC50: 130 nM

MLN8054+++

IC50: 4 nM+

IC50: 172 nM

Danusertib (PHA-739358)+++

IC50: 13 nM+

IC50: 79 nM

AT9283++++ IC50: ~3.0 nM

JNJ-7706621+++

IC50: 11 nM

Hesperadin+++

Ki app: 4.6 nM

Bcr-Abl,FLT3

Phase 2

Inhibitor Name

DNA Methyltransferase

Decitabine++++ IC50: 1 ng/mL

RG108

++

IC50: 115 nM

SGI-1027+

IC50: 7.5 μM

Lomeguatrib+++

IC50: 5 nM

Azacitidine√

Zebularine√

Thioguanine√

Procainamide HCl√

Phase 1+

IC50: 61 nM

Abl,TrkA,RET

Phase 2

JAK3,JAK2,Abl1 (T315I)

Phase 2

CDK2/CyclinE,CDK2/CyclinA,CDK1/CyclinB

Inhibitor Name

IC50: 250 nM

TbAUK1

Pinometostat (EPZ5676)++++ Ki: 80 pM

IC50: 48 nM

SNS-314+++

IC50: 9 nM++

IC50: 31 nM

ENMD-2076+++

IC50: 14 nM+

IC50: 350 nM

PHA-680632++

IC50: 27 nM+

IC50: 135 nM

MK-5108 (VX-689)++++ IC50: 0.064 nM

CYC116+++

Ki: 8 nM+++

Ki: 9 nM

AMG-900+++

IC50: 5 nM+++

IC50: 4 nM

PF-03814735++++ IC50: 0.8 nM+++

IC50: 5 nM

CCT129202+

IC50: 42 nM+

IC50: 198 nM

TAK-901++

IC50: 21 nM++

IC50: 15 nM

CCT137690++

IC50: 15 nM++

IC50: 25 nM

MK-8745++++ IC50: 0.6 nM

FLT3 (D835Y),Abl (T315I),FLT3++++ IC50: 3.5 nM

Cytidine deaminase
Phase 4
Sodium channel

Phase 4阻害選択性

IC50: 15 nM+

Phase 4

Histone Methyltransferase+++++ IC50: 3.4 nM

Clinical Phase

LCK,Src,MEK1++

KW-2449

Other Targets

Phase 2++++ IC50: ~3.0 nM

Aurora A Inhibitor I (TC-S 7010)

GSK1070916

Clinical Phase
Phase 3++++ IC50: 0.37 nM

Barasertib (AZD1152-HQPA|AZD2811)

10

Aurora C

IC50: 14 nM

Thiomyristoyl++++ IC50: 14 nM

IC50: 20 μM

Daprodustat (GSK1278863)
Lificiguat(YC-1)

Clinical Phase

BCRP,MDH2

FG-2216+

Other Targets

IC50: 21 nM++++ IC50: 1 nM++++ IC50: 1 nM

KC7F2

PHD3

IC50: 4.4 μM

MK-8617

BAY 87-2243

Aurora B

+++

阻害選択性

HIF

LW 6

Aurora A

ENMD-2076 L-(+)-Tartaric acid++++ IC50: 3 nM
FLT3,RET,VEGFR3/FLT4+

IC50: 120 nM++++ IC50: 1 nM

IC50: 227 nM+++

IC50: 6.5 nM++

IC50: 19 nM++

Ki: 24 nM

GSK343+++

IC50: 4 nM

Phase 1

BIX 01294+

IC50: 2.7 μM

Phase 2

Tazemetostat (EPZ-6438)+++

Ki: 2.5 nM

3-deazaneplanocin A (DZNeP) HCl++++ Ki: 50 pM

Phase 1

UNC1999++++ IC50: 2 nM

Phase 1MM-102+

SGC 0946++++ IC50: 0.3 nM

Entacapone+

IC50: 151 nM

LLY-283++

IC50: 20 nM

p38α
FLT1,FAK,TrkA+

EPZ005687
Phase 1

FGFR1,PLK1,FLT3

VEGFR2,FLT3,CDK2/CyclinE

Histone Methyltransferase

Phase 1

Menin-MLL interaction

Other Targets

Clinical Phase
Phase 2

IC50: 0.4 μM

FLT1,Tie-2,SIK

Phase 1JNJ-64619178++++ IC50: 0.14 nM

JAK3,c-Src,YES1

Phase 1

PF-06726304++++ Ki: 0.7 nM

A-196

++

IC50: 25 nM

SGC2085++

IC50: 50 nM

Phase 4Phase 111阻害選択性Inhibitor Name

阻害選択性
Histone Methyltransferase

Menin-MLL interaction

MI-503MI-463

Other Targets

Clinical Phase

Inhibitor Name

Epigenetic Reader Domain++

IC50: 14.7 nM

I-BRD9++pIC50: 5.3++

IC50: 15.3 nM

PF-CBP1 HCl+

IC50: 125nM

PFI-4

++

IC50: 80 nM

OF-1

++

Kd: 100 nM

GSK1324726A (I-BET726)+++

IC50: 41 nM

EPZ020411 2HCl+++

IC50: 119 nM

MS049

++

IC50: 34 nM

CPI-1205++++ IC50: 2 nM

Amodiaquine dihydrochloride dihydrate++

Ki: 18.6 nM

PFI-3

++

Kd: 72 nM

HLCL-61 HCL+

IC50: 16.74 μM

MS436

++

Ki: <0.085 μM

GSK591+++

IC50: 4 nM

CPI-203+++

IC50: 37 nM

EPZ011989+++

IC50: 103 nM

GSK2801+

Kd: 136 nM

Chaetocin+

IC50: 0.8 μM

ABBV-744

√

MS023

+++

IC50: 4 nM

KG-501 (2-naphthol-AS-E-phosphate)√

SGC707++

IC50: 31 nM

Mivebresib(ABBV-075)

√

AMI-1

+

IC50: 3.0 μM

CPI-169++++ IC50: 0.24 nM

CPI-360+

IC50: 102.3 nM

GSK503+++

IC50: 8 nM

EPZ015666(GSK3235025)+++

Ki: 5 nM

UNC0379+

IC50: 7.3 μM

EI1

+++

Phase 2

Inhibitor Name

IC50: 13 nM
IC50: 446 nM

MI-3 (Menin-MLL Inhibitor)+

IC50: 648 nM++++ IC50: 2 nM+++

IC50: <2.5 nM

UNC0638++

IC50: <15 nM

GSK126+++

IC50: 9.9 nM

EPZ004777++++ IC50: 0.4 nM

JQ-EZ-05 (JQEZ5)√GSK3326595 (EPZ015938)√

UNC3866

√

GLP
GLP

CBX4 chromodomains,CBX7 chromodomains√

MI-136
LLY-507√

BRD4770√

IL-6,MYC

Phase 1++

IC50: 60 nM

OG-L002+++

IC50: 20 nM

JIB-04++

IC50: 290 nM

Daminozide+

IC50: 1.5 μM

CP2

+++

IC50: 29 nM

CPI-455 HCl++++ IC50: 10 nM

GSK2879552 2HCl+

Ki: 1.7 μM

ORY-1001 (RG-6016) 2HCl+++

IC50: 20 nM

GSK J1+++

IC50: 28 nM

GSK-LSD1 2HCl++++ IC50: 16 nM

SP2509++++ IC50: 13 nM

ML324

+

IC50: 920 nM

IOX1

++

IC50: 0.1 μM

Inhibitor Name
Epigenetic Reader Domain

Histone demethylase

GSK J4 HCl

Other Targets

Clinical Phase

PHF8
Phase 3Phase 2

阻害選択性

阻害選択性
Other Targets

Clinical Phase

Histone Acetyltransferase

C646

+++

Ki: 400 nM
IC50: ~25 μM(+)-JQ1+++

IC50: 33 nM

Curcumin++

I-BET151 (GSK1210151A)+

IC50: 0.5 μM

A-485++++ IC50: 0.06 μM

PFI-1 (PF-6405761)++

IC50: 98 nM

Anacardic Acid+++

IC50: 8.5 μM+

IC50: 47 μM√

I-BET-762+++

IC50: 35 nM

Phase 2

MG149

Apabetalone (RVX-208)+

IC50: 0.51 μM

Phase 3Remodelin

SGC-CBP30++++ IC50: 21 nM

Bromosporine++++ IC50: 0.29 μM

OTX015++++ EC50: 10-19 nM

UNC1215+++

IC50: 40 nM

UNC669+

IC50: 6 μM

SF2523+

IC50: 241 nM

AZD5153++++ IC50: 5 nM

EED226++

GSK6853++++ pIC50: 8.1

CPI-637+++

BI-9564++++ Kd: 5.9 nM

BI-7273++++ IC50: 19 nM

12Phase 4

Histone Acetyltransferase

Epigenetic Reader Domain
Inhibitor Name

p300/CBP

阻害選択性+

UNC0642

Clinical Phase

Histone Demethylase

MI-2 (Menin-MLL Inhibitor)

PFI-2 HCl

Other Targets

Other Targets

Nrf2,NF-κB,HDAC

Clinical Phase

Phase 4

PCAF(p300/CREB-binding protein-associated factor)

注釈：
Phase 2

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

DNA-PK,PI3Kα,PI3Kγ
Phase 1

Kd: 82 nM

IC50: 0.03 μM

13

Methylation

阻害選択性
Inhibitor Name

DNA Methyltransferase
詳細情報はP11に記載されています++

UNC0642++++ IC50: <2.5 nM

UNC0638+++

BRD4770

√

LSD1

PRMT

阻害選択性

阻害選択性

Inhibitor Name

G9a/GLP

Chaetocin

LSD1

Inhibitor Name

OG-L002++

IC50: 20 nM

LLY-283+++ IC50: 20 nM

PRMT5

ORY-1001 (RG-6016) 2HCl++

IC50: 20 nM

JNJ-64619178++++ IC50: 0.14 nM

GSK-LSD1 2HCl+++

IC50: 16 nM

SGC2085

SP2509++++ IC50: 13 nM

PRMT4

JMJD

+

GSK591++++ IC50: 4 nM

JMJD3

GSK J4 HCl+++

IC50: 60 nM

JIB-04++

IC50: 855 nM

JMJD2

++

JMJD

IC50: 290 nM

Daminozide

IC50: 1.5 μM

Clinical Phase+

IC50: 1.6 μM++

IC50: 920 nM++

IC50: 0.6 μM+++

IC50: 53 nM++

IC50: 34 nM++++

IC50: 83 nM++++ IC50: 4 nM++

IC50: 119 nM+

IC50: 1.8 μM

+++

EZH2
++

Ki: 24 nM

GSK343+++

IC50: 4 nM

Tazemetostat (EPZ-6438)++

Ki: 2.5 nM

UNC1999++++ IC50: 2 nM

PF-06726304++++ Ki: 0.7 nM

CPI-1205
EPZ011989+++

CPI-169

IC50: 0.1 μM

EZH1

+

+++ IC50: 30 nM++++ IC50: 2 nM+

IC50: 52 nM

Ki: <3 nM+++++ IC50: 0.24 nM

+++
+

EI1

++

IC50: 13 nM

GSK126+++

IC50: 9.9 nM

AMI-1

+

EPZ015666(GSK3235025)++++ Ki: 5 nM

GSK3326595 (EPZ015938)√

IC50: 8.8 μM

yeast Hmt1p

Phase 2

SETD

A-196

+++

IC50: 25 nM

Cyproheptadine hydrochloride sesquihydrate++

IC50: 1 μM

UNC0379+

IC50: 7.3 μM

PFI-2 HCl++++ IC50: 2 nM

Other Targets

5-HT2

Clinical Phase

MLL
Inhibitor Name

Menin-MLL interaction

MM-102

CPI-360
IC50: 8 nM++ IC50: 119 nM

阻害選択性
IC50: 45 nM+++++++ IC50: 5 nM+++ IC50: 31 nM

Inhibitor NameKDM4E,KDM5C,PHD2

IC50: 240 nM++

GSK503

IC50: 223 nM

阻害選択性

阻害選択性

EPZ005687+

IC50: 43 nM

SETD

EZH1/2
Inhibitor Name

Clinical Phase

Phase 3++++ IC50: 28 nM

ML324

Other Targets

PHF8++++ IC50: 10 nM

CPI-455 HCl

IOX1

IC50: 230 nM+

Other Targets++++ IC50: 29 nM

CP2

GSK J1

+++

JMJD1

PRMT3

Phase 1
IC50: 50 nM

SGC707

Inhibitor Name

PRMT8

IC50: 16.74 μM

MS023

阻害選択性

PRMT1

+++ IC50: 10 nM

HLCL-61 HCLdSU(VAR)3-9,Neurospora crassa DIM5

IC50: <15 nM

PRMT6

++

EPZ020411 2HCl
MS049

Other Targets

IC50: 2.5 μM

JQ-EZ-05 (JQEZ5)

Phase 2MLL+++

MI-503++++ IC50: 14.7 nM

IC50: 103 nM

MI-463+++

IC50: 15.3 nM

IC50: 6.1 nM

MI-2 (Menin-MLL Inhibitor)++

IC50: 446 nM

IC50: 102.3 nM

MI-3 (Menin-MLL Inhibitor)+

IC50: 648 nM

MI-136√

IC50: 0.4 μM

COMT

√

阻害選択性

G9a/GLP

Inhibitor Name

阻害選択性
Inhibitor Name

G9a/GLP

BIX 01294+

IC50: 2.7 μM

A-366

+++

IC50: 3.3 nM

14

COMT

Clinical Phase

Entacapone++

IC50: 151 nM

Phase 4

Tolcapone+++

Ki: 30 nM

Phase 4

Other Targets

15

Immunology & Inflammation

DOT1
阻害選択性
Inhibitor Name

DOT1L

Pinometostat (EPZ5676)++++ Ki: 80 pM

SGC 0946+++

IC50: 0.3 nM

EPZ004777++

IC50: 0.4 nM

Clinical Phase
Phase 2T cellTh1

LPS

Nucleus

Cytokines(IL-1β, etc)

HNMT

Th1 CellTh2 cytokines (eg.IL-4)

IL-2, IFN-γ

NFAT

阻害選択性

Th2 Cell

NF-κB

AP-1

IL-R

Inhibitor Name

HNMT

Amodiaquine dihydrochloride dihydrate

+++

TNF

TLR

Ki: 18.6 nM

IL-1R

IL-12, IL-18,
TNF, etc

IKKγ

TNFR

SMYD2

MAPK
PKC

Calcineurin

阻害選択性
Inhibitor Name

PD-1/2

MyD88

SMYD2

LLY-507

√

IκBα

WDR5

PD-L1/2

Ub

IKKβ

P

P

MHCⅡ
TLR3, 7, 8, 9

TAB/TAK
Complex

MHCⅡ

Ag

阻害選択性
Inhibitor Name

WDR5

OICR-9429+++

Other Targets

Kd: 93 nM

Wdr5-MLL interaction

P

IκB

Ub

p50

MKKs

p65

Tyrosine
Phosphorylation
Cascade

ERK

P

JNK

p38

Pathogens

BCR

P

NF-κB

SAM MTase
+++

P

Syk

P

NucleusCXCL12CXCR4INFγ

PPMTase+++Ki: 2.6 μM

注釈：

MyD88

p38

ERK

IL-12, IFNα,
IFNβ, etc

JNK

B cellNrf2

IRFs

Nucleus

IRFs

Anti-oxidant
Genes

FOS

NF-κB

阻害選択性
Inhibitor Name

STAT

Dendritic CellBTKBCR Signaling

PPMTasefragments

MAPKKK

IL-R
IL-10, IL-3, etc

Inflammation,
Immune Regulation

IC50: 40 nM

MHCⅡ
TLR3, 7, 8, 9

Lyn

SAM MTase

Adenosine Dialdehyde (ADOX)

MHCⅡ

TLR

阻害選択性
Inhibitor Name

AntigenCapturing

CXCR1

TCR

TCR
IKKγ

Salirasib

cyt

)

N-γ

g.IF

s (e

e
okin

pro-IL-1β,
TNF, etc

IL-23-p19

Clinical Phase
Phase 2

PD-1/PD-L1
阻害選択性

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

16

Inhibitor Name

PD-1/PD-L1 interaction

Durvalumab++++ IC50: 0.1 nM

Atezolizumab+++

Kd: 0.4 nM

Nivolumab+++

IC50: 2.52 nM

PD-1/PD-L1 Inhibitor 3++

IC50: 5.6 nM

PD-1/PD-L1 inhibitor 1++

IC50: 0.006 μM

BMS202 (PD-1/PD-L1 inhibitor 2)+

IC50: 0.018 μM

Spartalizumab√

Camrelizumab√

AUNP-12√Pembrolizumab√

Other Targets
PD-L1/CD80

PD-1/PD-L2 interaction

17

COX

CCR

阻害選択性

阻害選択性

Inhibitor Name

COX

COX-1

Celecoxib

COX-2

Other Targets

Clinical Phase

Inhibitor Name

CCR

Phase 4

Maraviroc++

IC50: 3.3 nM

Phase 4

DAPTA

+++

IC50: 0.06 nM

Phase 2

Ibuprofen+

IC50: 13 μM+

IC50: 370 μM

Phase 4

Indomethacin++

IC50: 0.28 μM+

IC50: 14 μM

Phase 4++++ IC50: 18 nM

Phase 4

Diclofenac Sodium+++

IC50: 60 nM+++

IC50: 200 nM

Phase 4

Histamine Receptor

Lumiracoxib++

Ki: 3 μM+++

Ki: 60 nM

Phase 4阻害選択性

Lornoxicam++++ IC50: 5 nM++++ IC50: 8 nM

Phase 4

Naproxen Sodium+

IC50: 8.7 μM+

IC50: 5.2 μM

Phase 4

Ketorolac++

IC50: 1.23 μM++

IC50: 3.50 μM

Phase 4

Rofecoxib

Valdecoxib++++ IC50: 5 nM

Tolfenamic Acid+++

IC50: 0.2 μM+++

IC50: 150 nM+

IC50: 26 μM++

IC50: 0.78 μM++

IC50: 3.8 μM+++

IC50: 50 nM

Amfenac Sodium Monohydrate++

IC50: 250 nM+++

IC50: 0.11 μM

Nimesulide
Indometacin Sodium
NS-398 (NS398)++++ IC50: 40 nM

Meclofenamate Sodium

Phase 4Phase 1

Nepafenac

Phase 4

Sulindac√Phase 3

Meloxicam√

Phase 4√

Aspirin√Suprofen√

Piroxicam

IL receptor

Phase 4Phase 4Phase 4√

Ketoprofen

Phase 4√

Etodolac√Phase 4

Ibuprofen Lysine√

Phase 1

Pranoprofen√

Phase 4√

Asaraldehyde
Zaltoprofen
Acemetacin√

Nabumetone

Phenacetin

Phase 1√

Phenidone

√

PDE4

√

Phase 4

√
√

p300
√

√

Ethylene biosynthesis

Phase 4

Xanthohumol√

Phase 1

Oxaprozin√

Phase 1

Mefenamic Acid√

Phase 4

Ampiroxicam√

Flunixin Meglumin√

Salicin
Rutaecarpine√√

Other Targets

Clinical Phase
Phase 3+

IC50: 4 μM

Phase 4

Bepotastine Besilate+

pIC50: 5.7

Phase 4

Desloratadine++

IC50: 51 nM

Phase 4+++

IC50: 9.2 nM

Mizolastine+++

IC50: 47 nM

Phase 1Chlorpheniramine Maleate+++

IC50: 12 nM

Phase 4

Fexofenadine HCl++

IC50: 246 nM

Phase 4

Tripelennamine HCl+

IC50: 30 μM+++

IC50: 10 nM-19 nM++

Ki: 102 nM++++ IC50: 0.9 nM

Hydroxyzine 2HCl

AChE++++ Ki: 4.5 nM

Rupatadine Fumarate
Azatadine dimaleate

+++

PAFR

IC50: 6.5 nM++++ Ki: 1.3 nM

Bilastine+++

Phase 4

Ki: 44.15 nM

S 38093++++ pKi: 8.5

Alcaftadine++

Roxatidine Acetate HCl+√

Azelastine HCl√++

Ki: 1.2 μM+

IC50: 1.9 μM

pKi: 7.2

Betahistine 2HCl

Latrepirdine 2HCl

H4 receptor

Phase 4Phase 4

IC50: 3.2 μM
5-HT,GluR

Phase 3Phase 4Phase 4√Phase 4√Diphenhydramine HCl

Phase 4Cholinergic

Emedastine

Cetirizine DiHCl

Phase 4Phase 4

JNJ-7777120√

Phase 4√Phase 3√Phase 4√

Lafutidine√

Phase 3

Cimetidine√

Phase 3

Ebastine

Phase 4√

Buclizine HCl√

Cyproheptadine HCl√

Cholinergic
Phase 4

Ketotifen Fumarate√

Phase 4

Brompheniramine hydrogen maleate√

Phase 3Olopatadine HCl

Phase 4√

Emedastine Difumarate√

Triprolidine Hydrochloride√

Levocetirizine Dihydrochloride√

CarbinoxaMine Maleate√

Doxylamine Succinate√

Cyclizine 2HCl√

Levodropropizine

Phase 3Phase 2√

Famotidine
Hesperetin

Phase 3√Pemirolast potassium

18

H4 receptor++++ IC50: 3 nM

Meclizine 2HCl

LOX

Parecoxib
Salicylic acid

GABA receptor

H3 receptor

Loratadine

Epinastine HCl

Etoricoxib
Diflunisal√√

Deracoxib

H2 receptor

Clemastine Fumarate

Mianserin HCl
Phase 4√

Niflumic acidH1 receptor

Ranitidine Hydrochloride√

Bromfenac Sodium

Histamine receptor

Nizatidine
Phase 4√

Dexamethasone Sodium Phosphate

Inhibitor Name

Ciproxifan Maleate++++ IC50: 30 nM

Carprofen

Clinical Phase++++ IC50: 40 nM

Phase 4

√
√

TGF-β

19

IL Receptor

NADPH-oxidase

阻害選択性

阻害選択性

Inhibitor Name

Other Targets

IL Receptor

Dexamethasone (DHAP)√

Dexamethasone Sodium Phosphate√

Dexamethasone Acetate√

Clinical Phase

COX-2

Inhibitor Name

NOX1Phase 42-Acetylphenothiazine (ML171)+++

Phase 4

GKT137831++++ Ki: 110 nM

Phase 4

Apocynin

IC50: 0.25 μM

NOX4
++

IC50: 5 μM+++

Ki: 140 nM

NADPH-oxidase

Other Targets

Clinical Phase

NOX3,NOX2,xanthine oxidase
Phase 2+

IC50: 10 μM

Phase 1

注釈：

gp120/CD4

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

阻害選択性
Inhibitor Name

gp120/CD4

BMS-378806+++

YYA-021√

EC50: 0.85 nM-26.5 nM

CXCR
阻害選択性
Inhibitor Name

CXCR1

CXCR2

CXCR4

Other Targets

Clinical Phase

Plerixafor 8HCl (AMD3100 8HCl)

IC50: 0.25 μM++

IC50: 44 nM

CXCL12Phase 4

Plerixafor (AMD3100)

Ki: 110 nM++

IC50: 44 nM

CXCL12Phase 4

WZ811++++ EC50: 0.3 nM

SB225002+++

IC50: 22 nM

Tannic acid
Reparixin (Repertaxin)

Phase 3√Phase 3CXCL8√AMD3465 hexahydrobromide

√

MALT
阻害選択性
Inhibitor Name

MALT1

MI-2 (MALT1 inhibitor)+++

IC50: 5.84 μM

LTR
阻害選択性
Inhibitor Name

LTR

Zafirlukast√

Montelukast Sodium

√

MK571

√

Other Targets

Clinical Phase
Phase 2Phase 4

MRP1,cMOAT,MRP4

NOS
阻害選択性
Inhibitor Name

nNOS

eNOS

L-NAME HCl+++

Ki: 15 nM+++

Ki: 39 nM

1400W 2HCl++

Ki: 2 μM+

Ki: 50 μM

Agmatine sulfate

20

iNOS

Clinical Phase
Phase 3++++ Kd: <7 nM√

21

Protein Tyrosine Kinase
KinaseFibronetin

F
C

Cysteine Rich
Leucine Rich

L

Cadherin

F

C

C

C

F

F

F

C

Inhibitor Name

Ⅴ

Ⅳ

Ⅲ

Ⅱ

Ⅰ

IG-Like
Glycine Rich

EGF-Like
Acid Box

E
A

阻害選択性

E
E

F

C

E

F

L
A

F
F

C

F

C

F

F

F

F

F

VEGFR2++++ IC50: 3 nM

Vatalanib (PTK787) 2HCl+

IC50: 77 nM

RAF265 (CHIR-265)

F

C

Ⅵ

F

Ⅶ

VEGFR1

Linifanib (ABT-869)

F

C

C

EGFR

2/ErbB2

HER
ErbB3
ErbB4

FGFR

PDGFR

VEGFR

CSF-1R
Kit

TrkA
TrkB
TrkC

Tie
Tie-2

FLT3

Pan-FGFR Inhibitors
BGJ398AZD4547
Nintedanib
bitorsSelective FGFR Inhi )PD173074 (FGFR1)
SSR128129E (FGFR1

bitorsHER2 Inhi ib
Lapatin
714
24
-7
CP
Mubritinib
Neratinib
AZD8931Afatinib
Inhibitors
Pan-ErbB inib
Afat
Canertinib
Lapatinib
AZD8931 bitors
ErbB Inhi
tiv
Selec e (EGFR/ErbB1)
Erlotinib (HER2/ErbB2)
CP-724714

rsPan-IGF-1R Inhibito
OSI-906
NVP-AEW541
GSK1904529A
Inhibitors
Selective IGF-1R-1R)
NVP-ADW742 (IGF )-1R(IGF
AG-1024

Pan-PDGFR Inhibitors
Imatinib
Crenolanib
CP-673451
Selective PDGFR Inhibitors
Sunitinib (PDGFRβ)
TSU-68 (PDGFRβ)c-Kit Inhibitors
Masitinib
Dovitinib
Amuvatinib
OSI-930
Imatinib

Pan-VEGFR
Inhibitors
Axitinib
Nintedanib
Rego
Selective VE rafenib
GF
ZM 306416 R Inhibitors
Cabozantinib(VEGFR1)
SAR131675 (VEGFR2)(VEGFR3)

c-Met Inhibi
tors
Crizotinib
Foretinib
PHA-665752
BMS-777607

Eph
Eck
Eek
Erk
Elk

Ros

Ret

Ltk
ALK

PDK-1
Akt
PI3K/Akt
Pathway

Syk

ReceptoGNF-58 r Inhibitors
BMS-754 37
Selectiv
80
e Trk R 7
eceptor
Inhi
GW4417 bitor
56 (TrkA
)

c-RET
In
Regorahibitors
Danus fenib
TG101ertib
209

Tie-2
Tie2 kinaInhibitors
se
Cabozaninhibitortin
MGCD-2 ib
65

Bcr-Abl
c-Src

Ras

PKC

ALK Inhib
Alectin itors
Ceritin ib
AP2611ib
Crizoti 3n
TAE68 ib
4

IKK

c-Jun

Raf

JAK

c-Fos

ROCK

+

IC50: 660 nM

PDGFRβ,c-Kit,c-Fms

Phase 3

EC50: 30 nM

B-Raf

Phase 2+++

IC50: 6.5 nM

Phase 3

IC50: 6 nM

Kit,RET,PDGFR

Phase 3

IC50: 22 nM++++ IC50: 4.0 nM+++

IC50: 5.2 nM

PDGFRβ,FGFR1,PDGFRαPhase 4

IC50: 380 nM

++

FGFR1

Phase 3

Lenvatinib (E7080)++

Brivanib (BMS-540215)+

Glesatinib (MGCD265)++++ IC50: 3 nM

AEE788 (NVP-AEE788)+

IC50: 59 nM+++

IC50: 8 nM

IC50: 25 nM

IC50: 58.2 nM

FLT3,RET,Aurora A

Phase 2

IC50: 9 nM

CSF-1R,LCK,C-Raf

Phase 1CYC116+

Ki: 44 nM

Aurora A,Aurora B,FLT3

Phase 1

Ki8751++++ IC50: 0.9 nM

Telatinib+++

IC50: 6 nM++++ IC50: 4 nM

c-Kit,PDGFRαPhase 2

IC50: 10 nM++

IC50: 30 nM+

IC50: 47 nM

c-Kit,PDGFR,FGFR

Phase 4

KRN 633+

IC50: 170 nM+

IC50: 160 nM+

IC50: 125 nM

PDGFRα,c-Kit,BTK++

IC50: 23 nM+++

IC50: 8 nM

Dovitinib (TKI-258) Dilactic Acid

FLT3,c-Kit,FGFR1

Phase 3

Apatinib mesylate++++ IC50: 1 nM

RET

Phase 4

BMS-794833++

IC50: 15 nM

Met

Cabozantinib malate (XL184)++++ IC50: 0.035 nM+++

Brivanib Alaninate (BMS-582664)

IC50: 10 nM+++

IC50: 13 nM

IC50: 25 nM

FGFR1

Phase 3++

IC50: 16 nM

c-Met

Phase 2

Semaxanib (SU5416)+

IC50: 1.23 μM

ZM 323881 HCl++++ IC50: <2 nM+

IC50: 380 nM

Src,Abl+

IC50: 58.2 nM++++

IC50: 33 nM+

IC50: 35 nM++++ IC50: 0.5 nM

Nintedanib Ethanesulfonate Salt++

IC50: 34 nM+++

IC50: 13 nM

+++

+++

IC50: 5 nM+++

IC50: 13 nM+++

IC50: 6 nM

RETPhase 4c-Kit,PDGFRβ,FGFR1

Phase 3++++ IC50: 0.2 nM++++ IC50: 0.7 nM

c-Kit

Phase 4

RET,Raf-1,murine VEGFR2++

IC50: 17 nM+++

IC50: 5 nM

IC50: 820 nM+++

IC50: 9 nM

IC50: 80 nM

阻害選択性

Dovitinib (TKI258) Lactate+++

IC50: 13 nM

LY2874455+++

IC50: 7 nM

SKLB1002++

IC50: 32 nM

AZD2932+++

IC50: 8 nM

Sunitinib Malate+

IC50: 80 nM

FLT3,Kit,PDGFRβPhase 4

Cabozantinib (XL184, BMS-907351)++++ IC50: 0.035 nM

c-Met

Phase 4

Ponatinib (AP24534)++++ IC50: 1.5 nM

Abl,PDGFRα,FGFR1

Phase 3Axitinib++++ IC50: 0.1 nM++++ IC50: 0.18 nM++++ IC50: 0.1 nM-0.3 nM

PDGFRβ,Kit,PDGFRαPhase 3Foretinib (GSK1363089)+++

IC50: 6.8 nM++++ IC50: 0.86 nM++++ IC50: 2.8 nM

Met,Tie-2,RON

Phase 2+

IC50: 40 nM+

IC50: 110 nM

EGFR

Phase 4

Nintedanib (BIBF 1120)++

IC50: 34 nM+++

IC50: 13 nM+++

IC50: 13 nM

LCK,FLT3,FGFR2

Phase 4

Regorafenib (BAY 73-4506)+++

IC50: 13 nM+++

IC50: 4.2 nM+

IC50: 46 nM

RET,Raf-1,Kit

Phase 4

Pazopanib HCl (GW786034 HCl)
Cediranib (AZD2171)

+++
+++

IC50: 10 nM
IC50: 5 nM

PD173074
Dovitinib (TKI-258, CHIR-258)22++++++ IC50: 0.5 nM++++

IC50: 10 nM

IC50: 30 nM++++

IC50: 47 nM++++ IC50: <=3 nM

c-Kit,PDGFRβ,FGFR1

Phase 4Phase 3

FGFR1

IC50: 100 nM-200 nM
IC50: 13 nM

FGFR,PDGFR,c-Kit+++

IC50: 8 nM

FLT3,c-Kit,FGFR1

Phase 3Phase 3
FGFR2,PDGFRα,PDGFRβ++++ IC50: 2 nM

sumoylation,Axl,IRAK4Phase 4

DDR2,EPHA3,Axl

Phase 2++++ IC50: 3 nM++++

IC50: 10 nM

Phase 2++++ IC50: <=3 nM

IC50: 20 nM

Phase 3

FLT3,RET,Aurora A++++ IC50: 0.5 nM+

Raf-1,B-Raf,B-Raf (V599E)

IC50: 13 nM++++ IC50: 1 nM++

IC50: 15 nM

IC50: 15.9 nM

Fruquintinib (HMPL-013)

Sunitinib++

Phase 3

IC50: 0.33 μM

2-D08

Sorafenib Tosylate

Phase 4+++

Regorafenib Monohydrate

Clinical Phasec-Met

Golvatinib (E7050)

SU5402

Vandetanib (ZD6474)

c-Kit,PDGFRα+++Anlotinib (AL3818) dihydrochloride

Other Targets

IC50: 15.9 nM++

Pazopanib

VEGFR
VEGFR3Phase 2+++

BAW2881 (NVP-BAW2881)

VEGFR2Phase 2

EGFR,HER2/ErbB2,c-Abl+

BFH772VEGFR1

Met,RON,Tie-2

IC50: 77 nM

Sitravatinib (MGCD516)

Inhibitor Name++++ IC50: 4 nM++++ IC50: 3 nM+

Cediranib Maleate

JAK/STAT
Pathway

STAT

IC50: 37 nM

++

+++

Apatinib

Cell Cycle

GSK-3

MAPK
Pathway

NF-κB
Pathway

Rho

JAK

+

++++ IC50: 3 nM++++ IC50: 2 nM

IC50: 30 nM

ENMD-2076 L-(+)-Tartaric acid

PAK

Phase 3

EphB2,PDGFRα,PDGFRβMotesanib Diphosphate (AMG-706)

ZM 306416

PLC

CSF-1R,FLT3,Kit

SAR131675

Pan-Trk

Clinical Phase

IC50: 190 nM

IC50: 15 nM++

OSI-930

Met
Ron
Sea

Other Targets+++

Tivozanib (AV-951)

ENMD-2076

INSR
IGF-1RIRR

VEGFR3++++ IC50: 4 nM

Phase 2
IC50: 420 nM+

C-Raf-1,B-RAFV599E,c-Abl
FGFR1,PDGFRβ+++

IC50: 8 nM

c-Kit,FLT3 ,PDGFRβPhase 4

FLT3,c-Kit,FGFR1

Phase 3

FGFR2,FGFR1,FGFR4

Phase 1PDGFRβ,Flt3,c-Kit

EGFR
阻害選択性
Inhibitor Name

EGFR/ErbB1

HER2/ErbB2

ErbB3

ErbB4

mutant EGFR

Other Targets

Clinical Phase
Phase 4

Erlotinib HCl (OSI-744)++++ IC50: 2 nM

Gefitinib (ZD1839)++

IC50: 26 nM

Lapatinib (GW-572016) Ditosylate++

IC50: 10.8 nM+++

IC50: 9.2 nM+

Afatinib (BIBW2992)++++ IC50: 0.5 nM++

IC50: 14 nM++++ IC50: 1 nM

Neratinib (HKI-272)+

IC50: 92 nM+

IC50: 59 nM

Phase 4Phase 4

IC50: 367 nM

Phase 4
KDR,SrcPhase 323

PDGFR

阻害選択性
Inhibitor Name

EGFR/ErbB1

Canertinib (CI-1033)++++ IC50: 1.5 nM+++

IC50: 9.0 nM

Lapatinib++

IC50: 10.8 nM+++

IC50: 9.2 nM

AG-490 (Tyrphostin B42)+

IC50: 0.1 μM

CP-724714

HER2/ErbB2++

IC50: 10 nM+

IC50: 45.7 nM

Dacomitinib (PF299804, PF299)+++

WZ4002++++ IC50: 2 nM

Sapitinib (AZD8931)+++

IC50: 4 nM+++

IC50: 3 nM

CUDC-101+++

IC50: 2.4 nM++

IC50: 15.7 nM

AG-1478 (Tyrphostin AG-1478)+++

IC50: 3 nM

PD153035 HCl++++ Ki: 5.2 pM

Pelitinib (EKB-569)+

AEE788 (NVP-AEE788)
AC480 (BMS-599626)++

IC50: 6.0 nM

IC50: 38.5 nM

ErbB3

ErbB4

mutant EGFR

Other Targets

Phase 2+Phase 4

IC50: 367 nM

Phase 2++++Phase 3

IC50: 73.7 nM

Phase 2

IC50: 4 nM
HDAC,HDAC1,HDAC6

IC50: 1.255 μM++++ IC50: 2 nM+++

IC50: 6 nM+

IC50: 160 nM

IC50: 20 nM++

IC50: 30 nM+

IC50: 190 nM

AP26113-analog (ALK-IN-1)

Src,MEK/ERK,Raf

Phase 2c-Abl,FLT1,c-Fms

Phase 2Phase 1++

IC50: 36.8 nM

ALK,IGF1R,INSR

OSI-420++++ IC50: 2 nM

WZ3146++++ IC50: 5 nM

AST-1306++++ IC50: 0.5 nM

Rociletinib (CO-1686, AVL-301)++

Ki: 21.5 nM

Varlitinib+++

IC50: 7 nM

Icotinib+++

IC50: 5 nM

TAK-285++

IC50: 23 nM

WHI-P154+++

IC50: 4 nM

Src,VEGFR,JAK3

Daphnetin+

IC50: 7.67 μM

PKA,PKCPD168393++++ IC50: 0.70 nM

CNX-2006++

IC50: <20 nM

Tyrphostin 9+

IC50: 460 μM

AG-18

+

IC50: 35 μM+++

IC50: 3.0 nM

Phase 3Phase 3++++ IC50: 2 nM

Phase 4++

IC50: 17 nM+

MEK1,Aurora B,LCK

IC50: 260 nM++

JAK3,BTK

Phase 3++++ IC50: 1.7 nM

Del19,L85R

Phase 2++

Cetuximab++++ Kd: 0.39 nM

Lifirafenib (BGB-283)++

IC50: 29 nM+

IC50: 495 nM

Nazartinib (EGF816, NVS-816)++

Ki: 0.031 μM++

Ki: 0.031 μM+

IC50: 43.7 nM+

IC50: 15.5 nM

Brigatinib (AP26113)++++ IC50: 0.4 nM++++ IC50: 2 nM

CL-387785 (EKI-785)++++ IC50: 370 pM

Poziotinib (HM781-36B)+++

IC50: 3.2 nM

Osimertinib (AZD9291)++

IC50: 11.44 nM

AZ5104++++ IC50: <1 nM

HER2-Inhibitor-1√

Genistein√

Naquotinib(ASP8273)√

Olmutinib (HM61713, BI 1482694)√

Butein√Chrysophanic Acid√

Imatinib Mesylate (STI571)

WT A-RAF,C-RAF(Y340/341D),BRAF(V600E)

Phase 1
Phase 2

ALK,ROS1,FLT3

Phase 3

IC50: 5.3 nM

Other Targets

IC50: 57 nM

IC50: 100 nM++++ IC50: 2 nM

Ponatinib (AP24534)++++ IC50: 1.1 nM

Axitinib++++

IC50: 100 nM+

IC50: 84 nM

Nintedanib (BIBF 1120)++

IC50: 5.0 nM

IC50: 59 nM++++ IC50: 1.6 nM++

IC50: 65 nM

Clinical Phase

Raf-1,VEGFR2/Flk1,B-Raf

Phase 3c-Kit,v-Abl

Phase 4

FLT3,Kit,VEGFR2

Phase 4

Abl,VEGFR2,FGFR1

Phase 3VEGFR1/FLT1,VEGFR2/Flk1,VEGFR3

Phase 3c-Kit,v-Abl

Phase 4VEGFR2,VEGFR3,LCK

Phase 4VEGFR1,VEGFR2,VEGFR3

Phase 4

Dovitinib (TKI-258, CHIR-258)+++

IC50: 27 nM

FLT3,c-Kit,VEGFR3/FLT4

Phase 3

Linifanib (ABT-869)++

IC50: 66 nM

VEGFR1/FLT1,CSF-1R,VEGFR2/KDR

Phase 3Crenolanib (CP-868596)++++ Kd: 2.1 nM

Masitinib (AB1010)+

IC50: 540 nM+

IC50: 800 nM

Kit,Lyn B,Abl1

Phase 3Tivozanib (AV-951)++

IC50: 40 nM++

IC50: 49 nM

VEGFR2,VEGFR3,EphB2

Phase 3Amuvatinib (MP-470)++

IC50: 40 nM

c-Kit (D816H),FLT3 (D835Y)

Phase 2VEGFR1,VEGFR2,VEGFR2/Flk1

Phase 3+++++ Kd: 3.2 nM

IC50: 84 nM

Orantinib (TSU-68, SU6668)+++

Phase 2

Ki: 8 nM

Phase 3CP-673451+++

IC50: 10 nM

Ki8751++

IC50: 67 nM

VEGFR2,c-Kit+++

IC50: 15 nM

c-Kit,VEGFR3,VEGFR2

Telatinib
PP121++++ IC50: 2 nM

Pazopanib+

VEGFR1,VEGFR2,VEGFR3

Phase 4+++

IC50: 27 nM

FLT3,c-Kit,FGFR1

Phase 3+++

IC50: 22 nM

c-Met,c-Met,c-Met

Phase 2

IC50: 84 nM+

IC50: 0.3 μM-0.5 μM

Tyrphostin 9+

IC50: 0.5 μM

c-Kit (Swiss 3T3),FGFR (Swiss 3T3)
EGFR

Nintedanib Ethanesulfonate Salt+++++

IC50: 59 nM++

IC50: 65 nM+++

IC50: 22 nM

VEGFR3,VEGFR2,VEGFR1
Flk-1/DFR

Ki: 5 nM

Regorafenib Monohydrate

RET,Raf-1,murine VEGFR2
c-Kit (D816V)

Phase 3c-Kit,FLT3 ,VEGFR2

Phase 4

IC50: 27 nM

FLT3,c-Kit,FGFR1

Phase 3++++ IC50: 4 nM

Flt3,VEGFR-2,c-Kit++++ IC50: 0.5 nM

Sunitinib++++ IC50: 2 nM

Dovitinib (TKI258) Lactate+++

AZD2932
Sennoside B

Phase 2

Hck,VEGFR,mTOR

Tyrphostin AG 1296

Toceranib phosphate++++ IC50: 1 nM√

Phase 4

IC50: 14 nM

Phase 4++++

Sunitinib Malate

Imatinib (STI571)

PDGFRβ++Avapritinib (BLU-285)++

Phase 2

IC50: 23.5 nM

Phase 3+++

IC50: 7 nM

ACK1,BLK,BRK√

WZ804024

IC50: 823.3 nM

Phase 3++PDGFRαMK-2461++++ IC50: 0.18 nM

Gefitinib hydrochloride

PDGFR

Sorafenib Tosylate

Dovitinib (TKI-258) Dilactic Acid

PDGFR++++ IC50: 2 nM

Erlotinib

Phase 1

IC50: <20 nM

Lazertinib (YH25448,GNS-1480)

Afatinib (BIBW2992) Dimaleate

Inhibitor Name

Motesanib Diphosphate (AMG-706)++++ IC50: 0.8 nM

Avitinib (AC0010)++++ IC50: 0.3 nM

Phase 1

阻害選択性

Pazopanib HCl (GW786034 HCl)+AZD3759

Clinical Phase

topo II

Phase 4Phase 3BTK

mTOR

Phase 2

c-Met
阻害選択性
Inhibitor Name

c-Met

Other Targets

Clinical Phase

Crizotinib (PF-02341066)+

IC50: 11 nM

ALK

Phase 4

Cabozantinib (XL184, BMS-907351)+++

IC50: 1.3 nM

VEGFR2/KDR

Phase 4Foretinib (GSK1363089)++++ IC50: 0.4 nM

KDR,Tie-2,VEGFR3/FLT4

Phase 2

PHA-665752++

IC50: 9 nM

SU11274+

IC50: 0.01 μM

SGX-523+++

IC50: 4 nM

BMS-777607+++

IC50: 3.9 nM

Tivantinib (ARQ 197)+

Ki: 0.355 μM

Phase 3

JNJ-38877605+++

IC50: 4 nM

Phase 1

PF-04217903++

IC50: 4.8 nM

Glesatinib (MGCD265)++++ IC50: 1 nM

Capmatinib (INCB28060)++++ IC50: 0.13 nM

BMS-754807++

BMS-794833+++

RON,Flk1

Phase 1
Axl,RON,Tyro3

Phase 2Phase 1
RON,VEGFR2,VEGFR1

Phase 2

IC50: 5.6 nM

Insulin Receptor,IGF-1R,TrkB

Phase 2

IC50: 1.7 nM

VEGFR2

25

FLT3

阻害選択性
Inhibitor Name

c-Met

AMG-208++

MK-2461++++ IC50: 1.0 nM

Golvatinib (E7050)+

AMG-458++++ Ki: 0.5 nM

Tepotinib (EMD 1214063)+++

IC50: 4 nM

NVP-BVU972+

IC50: 14 nM

Savolitinib(AZD6094, HMPL-504)++

IC50: 5 nM

S49076++++ IC50: 1 nM

Merestinib (LY2801653)+++

AMG 337++++ IC50: 1 nM

NPS-1034+

Other Targets

Clinical Phase
Phase 2

IC50: 9 nM

IC50: 14 nM

c-Met (Y1235D),c-Met (Y1230C),c-Met (N1100)

Phase 2VEGFR2Phase 2Phase 2Phase 3
Mer,Axl,FGFR3
Phase 2

Ki: 2 nM

Phase 2

IC50: 48 nM

Axl

阻害選択性
Inhibitor Name

FLT3

Other Targets

Quizartinib (AC220)+++

Dovitinib (TKI-258, CHIR-258)++++ IC50: 1 nM

Amuvatinib (MP-470)+

Phase 2c-Kit,PDGFRβ,CSF-1R

Phase 2

TG101209

JAK2,RET,JAK3

KW-2449++++ IC50: 6.6 nM

ENMD-2076
Dovitinib (TKI-258) Dilactic Acid++++ IC50: 1 nM

Pacritinib (SB1518)
IC50: 42 nM

ENMD-2076 L-(+)-Tartaric acid++

IC50: 1.86 nM

HER2

Gilteritinib (ASP2215)++++ IC50: 0.29 nM

TAK-659++

阻害選択性

UNC2025++++ IC50: 0.8 nM

Other Targets

Clinical Phase

Lapatinib (GW-572016) Ditosylate+++

IC50: 9.2 nM

EGFR,ErbB4

Phase 4Afatinib (BIBW2992)++

IC50: 14 nM

EGFR (L858R),EGFR (wt),ErbB4

Phase 4

Neratinib (HKI-272)+

IC50: 59 nM

EGFR,KDR,Src

Phase 3Canertinib (CI-1033)+++

IC50: 9.0 nM

EGFR

Phase 2

Lapatinib+++

IC50: 9.2 nM

EGFR,ErbB4

Phase 4CP-724714++

IC50: 10 nM

Sapitinib (AZD8931)++++ IC50: 3 nM

CUDC-101++

Mubritinib (TAK 165)++++ IC50: 6.0 nM

AEE788 (NVP-AEE788)++++ IC50: 6 nM

EGFR,c-Abl,FLT1

Phase 2

AC480 (BMS-599626)+

IC50: 30 nM

HER1,HER4

Phase 1

TAK-285+

IC50: 17 nM

EGFR/HER1,HER4,MEK1

Phase 1Tyrphostin AG 879+

IC50: 1.0 μM

Trk

Lapatinib ditosylate monohydrate+++

IC50: 9.2 nM

EGFR,ErbB4

Irbinitinib (ARRY-380, ONT-380)+++

IC50: 8 nM

p95 HER2

Phase 2Afatinib (BIBW2992) Dimaleate++

IC50: 14 nM

EGFR (L858R),EGFR (wt),EGFR (L858R/T790M)

Phase 4

Poziotinib (HM781-36B)++++ IC50: 5.3 nM

HER1,HER4

Phase 2HER2-Inhibitor-1√

Pertuzumab√

Trastuzumab√

Phase 1

RET,Aurora A,VEGFR3/FLT4

Phase 2c-Kit,VEGFR3/FLT4,FGFR1

Phase 3

JAK2 (V617F),JAK2,TYK2

Phase 3

RET,Aurora A,VEGFR3/FLT4

Phase 2Phase 3Phase 2

Mer,Axl,Tyro3
CDK4

Dovitinib (TKI258) Lactate

Phase 3c-Kit,VEGFR3/FLT4,FGFR1

G-749++++ IC50: 0.4 nM

AZD2932

++

R406

√

Syk

Go6976√

JAK2,PKCα,PKCβ1

Mer,Aurora B,RETPDGFRβ,VEGFR-2,c-Kit

IC50: 7 nM

Phase 2

IC50: 15.7 nM

Phase 2

EGFR,HDAC,HDAC1

Phase 1

FGFR

Phase 1

阻害選択性

阻害選択性
IGF-1R

Insulin Receptor

Other Targets

Linsitinib (OSI-906)+++

IC50: 35 nM++

IC50: 75 nM

IRR

NVP-AEW541++

IC50: 0.15 μM++

IC50: 0.14 μM

FLT3,Tek,FLT1

GSK1904529A+++

IC50: 27 nM+++

IC50: 25 nM

NVP-ADW742+

IC50: 0.17 μM

BMS-536924++

IC50: 100 nM+++

IC50: 73 nM

AG-1024+

IC50: 7 μM+

IC50: 57 μM

GSK1838705A+++

IC50: 2 nM++++ IC50: 1.6 nM

ALK

BMS-754807++++ IC50: 1.8 nM++++ IC50: 1.7 nM

TrkB,Met,TrkA

PQ 401+

Picropodophyllin (PPP)++++ IC50: 1 nM

AZD3463√26

Abl (T315I),Abl,FGFR1

Syk,ZAP-70,JAK3

IC50: 4.6 nM

AMG 925

ErbB3,EGFR

IGF-1R
Inhibitor Name

Phase 3c-Kit (D816H),PDGFRα (V561D)

IC50: 81 nM

+

HER2

Phase 3c-Kit,VEGFR3/FLT4,FGFR1

Tandutinib (MLN518)

TCS 359

Inhibitor Name

Clinical Phase

IC50: 1.1 nM

Clinical Phase
Phase 3

Inhibitor Name

FGFR

FGFR1

FGFR2

FGFR3

Ponatinib (AP24534)++++ IC50: 2.2 nM

BGJ398 (NVP-BGJ398)++++ IC50: 0.9 nM

Nintedanib (BIBF 1120)+

IC50: 69 nM

PD173074++

IC50: ~25 nM

Dovitinib (TKI-258, CHIR-258)+++

IC50: 8 nM

AZD4547++++ IC50: 0.2 nM

Danusertib (PHA-739358)++

Brivanib (BMS-540215)+

Dovitinib (TKI-258) Dilactic Acid+++

IC50: 8 nM

MK-2461+

IC50: 65 nM

Brivanib Alaninate (BMS-582664)+

IC50: 148 nM

SSR128129E+

IC50: 1.9 μM

Derazantinib(ARQ-087)+++

IC50: 4.5 nM++++ IC50: 1.8 nM+++

IC50: 4.5 nM

Nintedanib Ethanesulfonate Salt+

IC50: 69 nM+++

IC50: 108 nM++++ IC50: 1.4 nM++++ IC50: 1.0 nM+

IC50: 60 nM+++

IC50: 108 nM+

IC50: 610 nM

IC50: 37 nM

IC50: <1 μM
Phase 3
ALK

Phase 2VEGFR3,VEGFR2,LCK

Phase 4Phase 3

KDR

Phase 3

IC50: 47 nM

Aurora A,Abl,TrkA

Phase 2

IC50: 148 nM

VEGFR2,Flk1,VEGFR1

Phase 3++

IC50: 39 nM

IC50: 9 nM++++ IC50: 1.8 nM+++

IC50: 9 nM

FLT3,c-Kit,VEGFR3/FLT4

Phase 3+

IC50: 50 nM

c-Met,c-Met,c-Met

Phase 2VEGFR2,Flk1,VEGFR1

Phase 3Phase 3

IC50: 37 nM++

IC50: 34 nM++++ IC50: <1.2 nM++++ IC50: 1.1 nM

PRN1371++++ IC50: 0.6 nM

PD-166866 (PD166866)+

IC50: 52.4 nM

S49076++

IC50: 18 nM

SU5402++

IC50: 30 nM

FIIN-2+++

IC50: 3.09 nM

Dovitinib (TKI258) Lactate+++

IC50: 8 nM

CH5183284 (Debio-1347)++

IC50: 9.3 nM

LY2874455++++ IC50: 2.8 nM++

IC50: 19.3 nM+++

IC50: 5 nM++++ IC50: 1.3 nM+++

IC50: 4.1 nM++++

IC50: 15 nM+

IC50: 150 nM++++ IC50: 3 nM++

IC50: 27 nM++

IC50: 45.3 nM+++

IC50: 9 nM

IC50: 7.6 nM++

IC50: 22 nM+

IC50: 290 nM++++ IC50: 2.6 nM+++

IC50: 6.4 nM+++

IC50: 6 nM

IC50: 17 nM

RET,DDR2,PDGFRβPhase 2VEGFR3,VEGFR2,VEGFR1

Roblitinib (FGF401)√

Phase 3

FLT3,c-Kit,VEGFR3/FLT4+++++++ IC50: 2.5 nM

H3B-6527

Erdafitinib (JNJ-42756493)

Clinical Phase

VEGFR2Phase 1
Phase 2
CSF1R

Phase 1

Phase 1
Met,Mer,Axl
VEGFR2,PDGFRβ

BLU9931

Phase 2Other Targets
Abl,PDGFRα,VEGFR2

BLU-554 (BLU554)

FAK,MEK,LCK

FGFR4

+++

+++

IC50: 4.3 nM

FLT3,c-Kit,VEGFR3/FLT4

Phase 3Phase 2VEGFR2Phase 1
Phase 327

c-Kit

ALK

阻害選択性

阻害選択性

Inhibitor Name

c-Kit

Other Targets

Clinical Phase

Inhibitor Name

ALK

Other Targets

Clinical Phase

Dasatinib++

IC50: 37 nM

Abl,SrcPhase 4

Crizotinib (PF-02341066)+

IC50: 24 nM

Imatinib Mesylate (STI571)+

IC50: 100 nM

PDGFR,v-Abl

Phase 4

TAE684 (NVP-TAE684)++

IC50: 3 nM

Axitinib++++ IC50: 1.7 nM

VEGFR1/FLT1,VEGFR2/Flk1,VEGFR3

Phase 3Alectinib (CH5424802)++

IC50: 1 nM

Pazopanib HCl (GW786034 HCl)+

VEGFR1,VEGFR2,VEGFR3

Phase 4

Ceritinib (LDK378)++++ IC50: 0.2 nM

Insulin Receptor,IGF-1R

Dovitinib (TKI-258, CHIR-258)++++ IC50: 2 nM

FLT3,VEGFR3/FLT4,FGFR1

Phase 3AP26113-analog (ALK-IN-1)++++ IC50: 0.07 nM

EGFR(C797S/del19),IGF1R,EGFR(del19)

Masitinib (AB1010)+

IC50: 200 nM

Lyn B,PDGFRα,PDGFRβPhase 3

GSK1838705A+++

IC50: 0.5 nM

Insulin Receptor,IGF-1R

Tivozanib (AV-951)++

IC50: 78 nM

VEGFR2,VEGFR3,EphB2

Phase 3

AZD3463+++

Ki: 0.75 nM

IGF-1R

Amuvatinib (MP-470)+++

IC50: 10 nM

PDGFRα (V561D),FLT3 (D835Y)

Phase 2

ASP3026+

IC50: 3.5 nM

Motesanib Diphosphate (AMG-706)+++

IC50: 8 nM

VEGFR1,VEGFR2,VEGFR3

Phase 3Alectinib hydrochloride++

IC50: 1.9 nM

OSI-930+

IC50: 80 nM

FLT1,KDR,CSF-1R

Phase 1

Ensartinib (X-396)+

IC50: <4 nM

Met

Ki8751++

IC50: 40 nM

VEGFR2,PDGFRαBelizatinib (TSR-011)+++

IC50: 0.7 nM

TrkC,TrkB,TrkA

Telatinib++++ IC50: 1 nM

VEGFR3,VEGFR2,PDGFRαPhase 2

TPX-0005++

IC50: 1.08 nM

Src

Phase 2

Pazopanib++

IC50: 74 nM

VEGFR1,VEGFR2,VEGFR3

Phase 4

Brigatinib (AP26113)+++

IC50: 0.37 nM

FLT3,IGF1R,EGFR(C797S/del19)

Phase 3

Dovitinib (TKI-258) Dilactic Acid++++ IC50: 2 nM

FLT3,FGFR1,VEGFR3/FLT4

Phase 3Lorlatinib (PF-6463922)++++ Ki: <0.02 nM

LTK (TYK1),FER,FES (FPS)

Phase 2Tyrphostin AG 1296+

IC50: 1.8 μM

PDGFR,FGFR (Swiss 3T3)

Entrectinib (RXDX-101)√

TrkB,TrkA,TrkC

Phase 3

Ripretinib (DCC-2618)+++

IC50: 8 nM

PDGFRRegorafenib Monohydrate+++

IC50: 7 nM

RET,Raf-1,murine VEGFR2

Avapritinib (BLU-285)++++ IC50: 0.5 nM

Sitravatinib (MGCD516)+++

Pexidartinib (PLX3397)
Dasatinib Monohydrate
Dovitinib (TKI258) Lactate++++ IC50: 2 nM

AZD2932+++

Sunitinib Malate√

FLT3,PDGFRβ,VEGFR2PDGFR inhibitor 1

√

PDGFR

Sunitinib√

FLT3 ,PDGFRβ ,VEGFR2

IC50: 140 nM

Phase 3

IC50: 6 nM

DDR2,EPHA3,Axl

Phase 2

Tie-2

+++

IC50: 10 nM

CSF-1R,Flt3

Phase 3阻害選択性++

IC50: 37 nM

Abl ,Src

Phase 4

FLT3,VEGFR3/FLT4,FGFR1

Phase 3

Inhibitor NamePDGFRβ,Flt3,VEGFR-2
Phase 4Tie-2

Other Targets

Clinical Phase

Met,RON,VEGFR2

Phase 2

p38 MAPK

Phase 1Glesatinib (MGCD265)+++

IC50: 7 nM

Tie2 kinase inhibitor++

IC50: 0.25 μM

Pexmetinib (ARRY-614)√

Inhibitor Name
Other Targets

Clinical Phase++++ IC50: 0.8 nM

Abl,c-Kit (D816V),c-Kit (wt)Phase 4

Saracatinib (AZD0530)++++ IC50: 2.7 nM

c-YES,EGFR (L861Q),
EGFR (L858R)

Phase 3

Bosutinib (SKI-606)++++ IC50: 1.2 nM

AblPhase 4Src

KX2-391++

GI50: 26 nM

NVP-BHG712+

IC50: 1.266 μM

PP2

Lck

+++ IC50: <4 nM++

IC50: 10 nM

Lyn

Yes

+++ IC50: 5 nM

Phase 3+++ IC50: 5 nM

IC50: 14 nM

PDGFR,Hck,VEGFR+++ IC50: 5 nM

MNS (3,4-Methylenedioxy-β-nitrostyrene,
MDBN)

+

Dasatinib hydrochloride++++ IC50: 0.8 nM

UM-164++++ Kd: 2.7 nM++

IC50: 6 nM

IC50: 29.3 μM

TPX-0005+++

IC50: 5.3 nM

CCT196969+

IC50: 0.03 μM

SU6656+

IC50: 280 nM

Dasatinib Monohydrate++++ IC50: 0.8 nM++

Fyn

EphB4,C-Raf,c-Abl+++ IC50: 4 nM

++

PP1

IC50: 6 nM

Kit,EGFR

Phase 3

p97,SykPhase 2Abl,c-Kit (D816V),c-Kit (wt)p38α,p38β
WT ALK,ALK(L1196M),
ALK(G1202R)++

Phase 2c-RET

Other Targets

Clinical Phase

Regorafenib (BAY 73-4506)++++ IC50: 1.5 nM

Raf-1,VEGFR2,Kit

Phase 4Danusertib (PHA-739358)++

IC50: 31 nM

Aurora A,Abl,TrkA

Phase 2

TG101209++

IC50: 17 nM

JAK2,FLT3,JAK3

Apatinib+++

IC50: 13 nM

VEGFR2

Regorafenib Monohydrate

Phase 4

Raf-1,murine VEGFR2,KIT

2-D08

+++

IC50: 11 nM

sumoylation,Axl,IRAK4

BMS-935177+

IC50: 110 nM

BTK,TEC,BLK

AD80++++ IC50: 0.4 nM

BAW2881 (NVP-BAW2881)+

Phase 4

Raf,S6 Kinase,Src
hVEGFR2,C-Raf-1,B-RAFV599E

IC50: 410 nM

TAM Receptor
阻害選択性

CRAF,V600E-BRAF,BRAF

IC50: 0.02 μM+

IC50: 170 nM+

IC50: 130 nM

Inhibitor Name++ IC50: 20 nM
Abl ,c-Kit (D816V),c-Kit (wt)Phase 4

BMS-777607

Mer++

IC50: 14 nM

R428 (BGB324)++++ IC50: 2 nM

AD80

√

S6 Kinase,Raf,RET V804M

Quercetin√

Sirtuin,PKC,PI3Kγ

UNC2250
Phase 4

AxL++++ IC50: 1.1 nM
++

Tyro3
+++

IC50: 4.3 nM+

IC50: 100 nM

Other Targets
RON,Met,FLT3

Clinical Phase
Phase 2Phase 2

IC50: 14 nM++++ IC50: 1.7 nM

sumoylation,IRAK4,ROS1

Phase 4++++ IC50: 0.73 nM

FLT3

Phase 3

DDR2,EPHA3,VEGFR3 (FLT4)

Phase 2c-Met,VEGFR2

Phase 1

2-D08
Gilteritinib (ASP2215)

28

Phase 3阻害選択性

Inhibitor Name

WH-4-023

Phase 1

c-RET

阻害選択性

PP121

Phase 2Phase 4

Src
Dasatinib

Phase 3Phase 3PDGFRα (D842V)

IC50: 9 nM

Phase 4c-Met

Sitravatinib (MGCD516)+++

IC50: 2 nM++++ IC50: 1.5 nM

RXDX-106 (CEP-40783)+

IC50: 29 nM+++

IC50: 7 nM++

IC50: 19 nM

29

阻害選択性

阻害選択性

Inhibitor Name

Mer

S49076+++

UNC2025++++ IC50: 0.74 nM

AxL

IC50: 2 nM

Tyro3

+++

IC50: 7 nM+

IC50: 27 nM++

TP-0903

Other Targets

Clinical Phase

Met,FGFR3,FGFR2
IC50: 17 nM

FLT3
Phase 2

Inhibitor Name

TrkB

TrkC

PF-06273340+++

IC50: 6 nM

TrkA++++ IC50: 4 nM++++ IC50: 3 nM

Sitravatinib (MGCD516)+++

IC50: 5 nM++

IC50: 9 nM++

Kd: 10 nM+

IC50: 12 nM

ANA-12++

IC50: 10.3 nM

GNF-5837++

LDC1267+++

IC50: <5 nM+

IC50: 29 nM++

IC50: 8 nM

Belizatinib (TSR-011)√

UNC2881+++

IC50: 4.3 nM+

IC50: 360 nM+

IC50: 250 nM

Larotrectinib (LOXO-101) sulfate

NPS-1034

Met

Entrectinib (RXDX-101)

CSF-1R

IC50: 8 nM

Trk receptor

Other Targets

Phase 1
DDR2,EPHA3,Axl+++

Clinical Phase

Phase 2

IC50: 7 nM
ALK
Phase 2√√

ALK,ROS1

Phase 3

ACK

阻害選択性
Inhibitor Name

CSF-1R

Other Targets

Clinical Phase

阻害選択性

Linifanib (ABT-869)+++

IC50: 3 nM

VEGFR1/FLT1,FLT3,VEGFR2/KDR

Phase 3

Inhibitor Name

OSI-930++

IC50: 15 nM

FLT1,KDR,LCK

Phase 1

XMD16-5√

GW2580+IC50: 30 nM

XMD8-87√

CEP-32496+++

Kd: 9 nM

RET,PDGFRβ,LCK

Pexidartinib (PLX3397)++

IC50: 20 nM

Kit,Flt3

BLZ945++++ IC50: 1 nM

Phase 3

TNK2

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

Phase 2

2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Ephrin receptor
阻害選択性
Inhibitor Name

Ephrin receptor

Other Targets

NVP-BHG712+++

C-Raf,c-Src,c-Abl

ED50: 25 nM

BTK
阻害選択性
Inhibitor NameBTK

Other Targets

Clinical Phase

Ibrutinib (PCI-32765)++++ IC50: 0.5 nM

BLK,Bmx,FGR

Phase 4

Spebrutinib (CC-292, AVL-292)++++ IC50: <0.5 nM

CNX-774+++

BTK inhibitor 1 (Compound 27)++++ IC50: 0.11 nM

ARQ 531+++

IC50: 0.85 nM

BRK,LCK,YES

BMS-935177++

IC50: 2.8 nM

TEC,BLK,BMX

ONO-4059 (GS-4059) hydrochloride+++

IC50: 2.2 nM

Olmutinib (HM61713, BI 1482694)+

IC50: 13.9 nM

Acalabrutinib (ACP-196)++

IC50: 3nM

ONO-4059 analogue+

IC50: 23.9 nM

LFM-A13+

Ki: 1.4 μM

RN486

++

IC50: 4 nM

CGI1746+++

IC50: 1.9 nM

Btk inhibitor 2√

Phase 2

IC50: <1 nM

Phase 1

Phase 1
Phase 2mutant EGFR

Phase 3Phase 3

Trk receptor
阻害選択性
Inhibitor Name

TrkA

BMS-754807++

GW441756++++ IC50: 2 nM

BMS-935177+

30

IC50: 7.4 nM

IC50: 30 nM

Other Targets

Clinical Phase+++

IC50: 4.1 nM

TrkB

TrkC

Trk receptor

Insulin Receptor,IGF-1R,Met

Phase 2+

IC50: 100 nM

BTK,TEC,BLK

31

Angiogenesis
TGF-β
TGF-R

VDA
阻害選択性
Inhibitor Name

Pan-FGFR Inhibitors
BGJ398AZD4547
Nintedanib
Selective FGFR Inhibitors
PD173074 (FGFR1)
SSR128129E (FGFR1)

Pan-VEGFR Inhibitors
Axitinib
Nintedanib
Regorafenib
Selective VEGFR Inhibitors
ZM 306416 (VEGFR1)
Cabozantinib (VEGFR2)
SAR131675 (VEGFR3)

VEGFR

S1P

FGFR

VDA

Other Targets

Clinical Phase

DMXAA (Vadimezan)++

Ki: 20 μM

Phase 2Plinabulin (NPI-2358)+++

IC50: 9.8 nM-18 nM

Phase 3Verteporfin√

YAP/TEAD interaction

Phase 4

S1PR

Bcr-Abl
阻害選択性

Pan-PI3K Inhibitors
BEZ235
GDC-0941
LY294002
Selective PI3K Inhibitors
HS-173 (p110α)
TGX-221 (p110β)
CZC24832 (p110γ)
CAL-101 (p110δ)ALK Inhibitors
Alectinib
Ceritinib
AP26113
Crizotinib
TAE684

ALK

Inhibitor Name
Dasatinib

PI3K

G-protein

Imatinib Mesylate (STI571)

S1P

Ras

PI3K/Akt
Pathway

TGF
Pathway

Src Inhibitors
Dasatinib
Saracatinib
Bosutinib
KX2-391

c-Src

eNOS

CAS

Pan-Raf Inhibitors
Vemurafenib
Sorafenib
Dabrafenib
Selective Raf Inhibitors
GDC-0879 (B-Raf)
GW5074 (C-Raf)NO
Angiogenesis

MAPK
Pathway

Bcr-Abl++++ IC50: 0.6 nM

HIF Inhibitors
2-Methoxyestradiol
BAY 87-2243
HIF modulators
Roxadustat
IOX2

Raf

HIF Protein

詳細情報はP22に記載されています

EGFR

詳細情報はP23に記載されています

HER2

詳細情報はP26に記載されています

FGFR

詳細情報はP27に記載されています

Src

詳細情報はP28に記載されています

BTK

詳細情報はP30に記載されています

32

JAK

詳細情報はP9に記載されています

PDGFR

詳細情報はP25に記載されています

FLT3

詳細情報はP27に記載されています

HIF

詳細情報はP10に記載されています

ALK

詳細情報はP29に記載されています

Other Targets

Clinical Phase

Src,c-Kit (D816V),c-Kit (wt)Phase 4c-Kit,PDGFR

Phase 4PDGFRα,VEGFR2,FGFR1

Phase 3+

Ponatinib (AP24534)++++ IC50: 0.37 nM

Nilotinib (AMN-107)++

IC50: <30 nM

Danusertib (PHA-739358)++

IC50: 25 nM

IC50: 600 nM++++ IC50: 0.37 nM

Phase 4

AT9283++

IC50: 25 nM

Aurora A,TrkA,RET

Phase 2+++

IC50: 4 nM

JAK3,JAK2,Aurora B

Phase 2Degrasyn (WP1130)+

IC50: 1.8 μM

Bafetinib (INNO-406)++

IC50: 5.8 nM++

IC50: 5.8 nM

LynPhase 2

KW-2449++

IC50: 14 nM+++

IC50: 4 nM

FLT3 (D835Y),FLT3,FGFR1

Phase 1+

IC50: 1.667 μM

EphB4,C-Raf,c-Src++

IC50: 18 nM

PDGFR,Hck,VEGFR+++

IC50: 4 nM

FLT3,KDR,Tie-2

DUB

NVP-BHG712
PP121

++

IC50: 18 nM

Rebastinib (DCC-2036)

VEGFR

Abl
++++ IC50: 0.6 nM

GZD824 Dimesylate(HQP1351)++++ IC50: 0.34 nM

GNF-2

+

IC50: 268 nM

Nilotinib hydrochloride++

IC50: <30 nM

Dasatinib hydrochloride++++ IC50: 0.6 nM++++ IC50: 0.6 nM

Asciminib (ABL001)++++ IC50: 0.45 nM++++ IC50: 0.45 nM

GNF-7

+++

IC50: <5 nM

Radotinib+

IC50: 34 nM

Dasatinib Monohydrate++++ IC50: 0.6 nM

GNF-5

+

IC50: 220 nM

PD173955+++

IC50: 1 nM-2 nM

Phase 2++++ IC50: 0.15 nM+

Src,c-Kit (D816V),c-Kit (wt)Phase 3

IC50: 133 nM
Phase 3++++ IC50: 0.6 nM

Src,c-Kit (D816V),c-Kit (wt)Phase 4

Src

Syk
阻害選択性
Inhibitor Name

Syk

Other Targets

Clinical Phase

Flt3

R406

++

IC50: 41 nM

R788 (Fostamatinib) Disodium++

IC50: 41 nM

R406 (free base)++

IC50: 41 nM

PRT062607 (P505-15, BIIB057) HCl++++ IC50: 1 nM

FGR,MLK1

Phase 2

Fostamatinib (R788)++

IC50: 41 nM

Adenosine A3 receptor,Adenosine transporter,
Monoamine transporter

Phase 3

MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)+

IC50: 2.5 μM

p97,SrcPhase 2

TAK-659++++ IC50: 3.2 nM

PRT-060318 2HCl++++ IC50: 4nM

Entospletinib (GS-9973)+++

IC50: 7.7 nM

RO9021+++

IC50: 5.6 nM

BAY-61-3606+++

Ki: 7.5 nM

Piceatannol√

Phase 3Phase 2

Lyn,cAK,PKC

33

Apoptosis

FAK
阻害選択性
Inhibitor NameFAKOther Targets

Clinical Phase

PF-00562271 Besylate++++ IC50: 1.5 nM

CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB

Phase 1PF-562271++++ IC50: 1.5 nM

CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB

PF-573228+

IC50: 4 nM

TAE226 (NVP-TAE226)++

IC50: 3.5 nM

Insulin Receptor,IGF-1R,c-Met

PF-03814735+

IC50: 22 nM

Aurora A,Aurora B,FLT1

PF-562271 HCl++++ IC50: 1.5 nM

GSK2256098++++ Ki: 0.4 nM

PF-431396++

PND-1186 (VS-4718)++++ IC50: 1.5 nM

Y15√Defactinib (VS-6063, PF-04554878)√

Solanesol (Nonaisoprenol)√

TNF-alpha Inhibitors
Lenalidomide
Pomalidomide
Thalidomide

TNF-α

Cytokine

Phase 1STAT

CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB

Caspase-8

Phase 2

Caspase Inhibitors
Belnacasan
Z-VAD-FMK
Caspase Activators
PAC-1
Apoptosis Activator 2

IC50: 2 nM
Phase 1

Caspase-3

PKC

IKKα

Survivin Inhibitor
YM155

cIAP
Caspase-9

Apaf1

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

Mdm2

2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。

IAP Inhibitors
Birinapant
GDC-0152
Embelin
BV-6
LCL1613.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

p53

Mdm2 Antagonists
Nutlin-3
Nutlin-3a
YH239-EE
Mdm2 Activator
NSC 207895

Raf

Src

Ras

PI3K

NF-κB

Phase 2JAK

NIK

ERK1/2

Bcl-xL

Bcl-2

CytC

Survivin

Bad

mTOR

c-Jun

GSK-3

Caspase-9
p70S6K

Caspase Inhibitors
Belnacasan
Z-VAD-FMK
Caspase Activators
PAC-1
Apoptosis Activator 2

Caspase-3

Bcl-xL
Bcl-2

Apoptosis

ATM

Akt
GSK-3

p53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μ

JNK

Akt

Pan-Bcl-2
Inhibitors
ABT-737
ABT-263
TW-37
Selective Bcl-2
Inhibitor
ABT-199 (Bcl-2)

DNA-PKDNA Damage

PD-1/PD-L1

c-RET

詳細情報はP17に記載されています

詳細情報はP29に記載されています

Bcl-2
阻害選択性
Inhibitor Name

Bcl-2

Bcl-B

Bcl-w

Bcl-xL

ABT-737+++ EC50: 30.3 nM + EC50: 1.82 μM+++ EC50: 197.8 nM +++ EC50: 78.7 nM

Navitoclax (ABT-263)++++ Ki: <=1 nM++++ Ki: <=1 nM

Obatoclax Mesylate (GX15-070)+++ Ki: 0.22 μM

TW-37

++

Mcl-1

Bax

Bfl-1

Other
Targets

Phase 2++++ Ki: <=0.5 nM

Phase 3

Ki: 0.29 μM+

Ki: 1.11 μM+++ Ki: 0.26 μM++

Ki: 0.48 μM+++ Ki: 0.18 μM+++ IC50: 0.20 μM

Phase 3

Venetoclax (ABT-199, GDC-0199) ++++ Ki: <0.01 nM
AT101

++

Ki: 0.32 μM

HA14-1+

IC50: 9 μM

Sabutoclax++

IC50: 0.32 μM++

IC50: 0.31 μM

BH3I-1+

Ki: 2.4 μM

A-1331852++++ Ki: <0.01 nM

A-1155463++++ Ki: <0.01 nM

A-1210477

p53/MDM2++++ IC50: 1.1 nM+

IC50: 1.06 μM++ IC50: 0.66 μM++++ IC50: 0.02 μM+

IC50: 1.47 μM

+

BTSA1

34

++ IC50: 0.62 μM++ Ki: 490 nM

WEHI-539

Marinopyrrole A (Maritoclax)

Phase 2+++ IC50: 26.2 nM

UMI-77

Gambogic Acid

Clinical Phase+ IC50: 1.06 μM Caspase

IC50: 0.79 μM
√

√

35

Caspase

Survivin

阻害選択性

阻害選択性

Inhibitor Name Caspase

Caspase-1

Belnacasan++++
Ki: 0.8 nM

Ac-DEVD-CHO+++
Ki: 18 nM

Caspase-8++++
Ki: 230 pM++++
Ki: 0.92 nM

Caspase-9++
Ki: 60 nM

Caspase-4 Capase-7 Caspase-2 Caspase-5 Caspase-6 Caspase-10 Clinical Phase

Inhibitor Name++++
Ki: <0.6 nM

YM155 (Sepantronium Bromide)++
Ki: 132 nM

Phase 2+++
Ki: 1.6 nM+
Ki: 1.71 μM++
Ki: 205 nM+++
Ki: 31 nM

Survivin+++

Clinical Phase

IC50: 0.54 nM

Phase 2+++
Ki: 12 nM

++
++
++
++
IC50: 25 nM-400 nM IC50: 25 nM-400 nM IC50: 25 nM-400 nM IC50: 25 nM-400 nM

Q-VD-Oph
Z-VAD-FMK

Caspase-3

IAP

√

阻害選択性

Z-IETD-FMK√

Emricasan√

Z-VAD(OH)-FMK√

Phase 2

Z-DEVD-FMK√

Inhibitor Name

cIAP

XIAP

Birinapant++++ Kd: <1 nM++

Kd: 45 nM

GDC-0152+++

Ki: 17 nM++

Ki: 28 nM

AT406 (SM-406)++++ Ki: 1.9 nM+

Ki: 66.4 nM

AZD5582++++++

IC50: 15 nM+

IC50: 4.1 μM

IC50: 15 nM

Embelin

p53

BV-6

√

LCL161√Other Targets

Clinical Phase
Phase 2Phase 1MLXBIR3SG

Phase 15-LO,mPGES-1

Phase 2

阻害選択性
Inhibitor Name

p53

Pifithrin-α (PFTα) HBr√

Pifithrin-μ√

ReACp53

√

PERK
阻害選択性
Inhibitor Name

TNF-alpha
阻害選択性
Inhibitor Name

TNF-α

Other Targets

PERK

GSK2606414++++ IC50: 0.4 nM

GSK2656157+++

IC50: 0.9 nM

ISRIB (trans-isomer)++

IC50: 5 nM

Salubrinal√

Clinical Phase
Phase 3

ASK

Pomalidomide+++

IC50: 13 nM

Necrostatin-1+

EC50: 490 nM

QNZ (EVP4593)++++ IC50: 7 nM

GSK'963++

IC50: 29 nM

Phase 4

Inhibitor Name

GSK2982772++++ IC50: 1 nM

Phase 2

Selonsertib (GS-4997)+++

pIC50: 8.3

Thalidomide√

E3 Ligase

Phase 4

NQDI-1++

IC50: 3 μM

Acetylcysteine√

ROS/ROS1

Phase 4

Adalimumab√

GSK481

√

阻害選択性

NF-κB

ASK1

Clinical Phase
Phase 2

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Mdm2
阻害選択性
Inhibitor Name

Mdm2
++

IC50: 180 nM

Nutlin-3a+++

IC50: 90 nM

Nutlin-3b+

IC50: 13.6 μM

MX69

++

Kd: 2.34 μM

NVP-CGM097++++ IC50: 1.7 nM

MI-773 (SAR405838)++++ Ki: 0.88 nM

Idasanutlin (RG-7388)+++

IC50: 6 nM

RG-7112+++

Kd: 11 nM

HDM201√

YH239-EE√

Nutlin-3
NSC 207895

36

MDMX

+

IC50: 2.5 μM

Other Targets

Clinical Phase

p53

p53

Phase 1
Phase 3Phase 237

Autophagy

LRRK2
阻害選択性
Energy Depletion

Stressp53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μ

IKKβ

Sestrins

Depletionof Amino Acids

AMPK

HIFs

Ras

PI3K

PTEN

MAPK
TSC 1/2

Pan-mTOR Inhibitors
AZD8055
KU-0063794
PP242
Selective mTOR Inhibitors
Rapamycin (mTORC1)
Everolimus (mTORC1)

Inhibitor Name

Limitation for Insulin,
Growth Factors, or Hormones

LKB1

p53

Hypoxia

Glucagon

RAGs

Pan-PI3K Inhibitors
BEZ235
GDC-0941
LY294002
Selective PI3K Inhibitors
HS-173 (p110α)
TGX-221 (p110β)
CZC24832 (p110γ)
CAL-101 (p110δ)

Akt

Rheb
mTORC1
ULK1 Complex

Ammonia
Autophagy Inhibitors
LY294002
Paclitaxel
Wortmannin
Autophagy Activators
Temozolomide
Metformin
Trifluoperazine

eEF-2
Kinase

Ca2+

FOXOs

LRRK2

Other Targets

LRRK2-IN-1++

IC50: 6 nM

DCLK2

GSK2578215A++

IC50: 8.9 nM

GNE-9605+++

IC50: 19 nM

GNE-7915+++

IC50: 9 nM

GNE-0877++++ Ki: 0.7 nM

URMC-099+

IC50: 11 nM

Abl1,MLK3,MLK1

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Pan-Akt Inhibitors
MK-2206
Perifosine
GSK690693
Selective Akt Inhibitors
A-674563 (Akt1)
CCT128930 (Akt2)

Autophagy
1 Regulation of Induction
P

Atg13 P
P

mTOR
P

P

2 Isolation Membrane

Atg13 Atg1 Atg17
ActiveAutophagosome

3

Atg13

5 Docking and Fusion

6 Vesicle Breakdown
and Degradation

Cathepsins
44 Retrieval

2 Vesicle Nucleation

Autolysosome

Lysosome

PI3K Complex III
UVRAG
Beclin-1
Vps34 P Bcl-2/Bcl-xL
Vps15
Atg9

3 Vesicle Elongation
Atg10 E2

Atg9
Atg18

Atg5

Atg4

P1

Atg12

Atg5
Atg16
Atg16
Atg16
Atg5
Atg16 Atg5
Atg12
Atg12

Atg12
Atg5

Atg12

Atg7 E1
LC3

LC3

Gly

Atg12

Atg5

Atg6

LC3
LC3

Atg3 E2

CXCR

詳細情報はP20に記載されています

Autophagy
阻害選択性
Inhibitor Name

Autophagy

EAD1+

IC50: 5.8 μM

Autophinib+++

IC50: 40 nM

MRT68921 HCl++++ IC50: 1.1 nM

SBI-0206965++

Valproic acid sodium salt (Sodium valproate)√

ROC-325

√

Lys05

√

Hydroxychloroquine Sulfate√

38

Other Targets

Clinical Phase

Vps34

IC50: 108 nM
HDAC,GABA receptor

Phase 4TLR9Phase 439

ER stress & UPR

JAK/STATPERK

Pan-Trk Receptor Inhibitors
GNF-5837
BMS-754807
Selective Trk Receptor
Inhibitor
GW441756 (TrkA)

ASK

詳細情報はP37に記載されています

詳細情報はP37に記載されています

Src Inhibitors
Dasatinib
Saracatinib
Bosutinib
KX2-391JNK

Pan-JAK Inhibitors
Ruxolitinib
Momelotinib
AT9283
Selective JAK Inhibitors
AZD1480 (JAK2)
Tofacitinib Citrate (JAK3)

Growth Factors

Tyk

JAK

Pan-PI3K Inhibitors
BEZ235
GDC-0941
LY294002
Selective PI3K Inhibitors
HS-173 (p110α)
TGX-221 (p110β)
CZC24832 (p110γ)
CAL-101 (p110δ)

阻害選択性
Src
Inhibitor Name

JNK1

JNK2

JNK3

SP600125+++

IC50: 40 nM+++

IC50: 40 nM++

JNK-IN-8++++ IC50: 4.7 nM+++

IC50: 18.7 nM++++ IC50: 1 nM

Tanzisertib(CC-930)++

IC50: 0.061 μM

IC50: 90 nM+++

IC50: 0.007 μM++++ IC50: 0.006 μM+

pIC50: 6.5++

BI-78D3JNK+

Clinical Phase

Aurora A,TrkA,FLT3

STAT

Kit (V559D,T670I),Kit (V559D)
Phase 2+JNK Inhibitor IX

IC50: 0.4 μM

Other Targets

IC50: 280 nM

MLK
√

p38

阻害選択性
HSP70

HSP90

HSP90αHSP90βHSP105

Other Targets

Clinical Phase
Phase 3

Tanespimycin (17-AAG)+++ IC50: 5 nM

Luminespib (AUY-922, NVP-AUY922)+++ IC50: 13 nM

Alvespimycin (17-DMAG) HCl+

IC50: 62 nM

Phase 2

Ganetespib (STA-9090)+++ IC50: 4 nM

Phase 3

BIIB021++++ Ki: 1.7 nM

Phase 2

Onalespib (AT13387)+++ IC50: 18 nM

Phase 2

Geldanamycin+

Kd: 0.78 μM

NVP-BEP800+

IC50: 58 nM

SNX-2112 (PF-04928473)++

Ka: 30 nM

PF-04929113 (SNX-5422)++

Kd: 41 nM

KW-2478++++ IC50: 3.8 nM

Phase 2

XL888++

IC50: 24 nM

Phase 1Apoptozole+

Kd: 0.14 μM

VER155008+

IC50: 0.5 μM+++ IC50: 13 nM

ERK1/2

p185++

Ka: 30 nM

IC50: 58 nM++

Ka: 30 nM+++ IC50: 21 nM

CH5138303++++ Kd: 0.48 nM

VER-49009

++

HER2

Phase 2

NMS-E973+++ DC50: <10 nM

PU-H71+

HSP990 (NVP-HSP990)++++ IC50: 0.6 nM+++ IC50: 21 nM++

IC50: 47 nM

Phase 1++++ IC50: 0.6 nM

Phase 1++++ IC50: 0.8 nM√

KNK437

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Pan-mTOR Inhibitors
AZD8055
KU-0063794
PP242
Selective mTOR Inhibitors
Rapamycin (mTORC1)
Everolimus (mTORC1)

√

Tyk

JAK

STAT

STAT

STAT
DNA

Pan-STAT Inhibitor
SH-4-54
Selective STAT Inhibitors
Fludarabine (STAT1)
S3I-201 (STAT3)
Cryptotanshinone (STAT3)

STAT
STAT
Pim1

Pim Inhibitors
SGI-1776
SMI-4aAZD1208
CX-6258

c-Myc

c-Myc Inhibitor
10058-F4

p21
Pan-CDK Inhibitors
Palbociclib
Roscovitine
Dinaciclib
Selective CDK Inhibitors
XL413 (CDK7)
LDC000067 (CDK9)

ISRE/GASJAK 詳細情報はP9に記載されています

CDK

Cell Growth, Survival,
Differentiation and Oncogenesis

Bcl-2

Pan-Bcl-2
Inhibitors
ABT-737
ABT-263
TW-37
Selective Bcl-2
Inhibitor
ABT-199 (Bcl-2)

EGFR 詳細情報はP23に記載されています

STAT
阻害選択性
STAT1

STAT3

S3I-201+

IC50: 86 μM

Stattic+

IC50: 5.1 μM

Niclosamide++

IC50: 0.7 μM

STAT5

STAT6

Other Targets

Clinical Phase

Phase 2

AS1517499

IC50: 51 nM

Cytokine

Pim 詳細情報はP10に記載されています++++ Kd: 0.48 nM

IC50: 47 nM

STAT

SOCS

Pan-JAK Inhibitors
Ruxolitinib
Momelotinib
AT9283
Selective JAK Inhibitors
AZD1480 (JAK2)
Tofacitinib Citrate (JAK3)mTOR

Phase 2+++ IC50: 21 nM+

Pan-STAT Inhibitor
SH-4-54
Selective STAT Inhibitors
Fludarabine (STAT1)
S3I-201 (STAT3)
Cryptotanshinone (STAT3)

Inhibitor Name

VER-50589

TRC051384

JNK

Pan-Akt Inhibitors
MK-2206
Perifosine
GSK690693
Selective Akt Inhibitors
A-674563 (Akt1)
CCT128930 (Akt2)

Akt

MKK1/2JNK Inhibitors
SP600125
JNK-IN-8JNK Inhibitor IX

HSP (e.g. HSP90)
Inhibitor Name

Raf

Rac

pIC50: 6.7

Vacquinol-1

PI3K

Ras

Pan-Trk Receptor Inhibitors
GNF-5837
BMS-754807
Selective Trk Receptor
Inhibitor
GW441756 (TrkA)++++ IC50: 21 nM

C188-9++++ Kd: 4.7 nM

BP-1-102+++

Kd: 504 nM

SH-4-54+++

Kd: 300 nM

Cryptotanshinone++

IC50: 4.6 μM

Fludarabine√

Nifuroxazide√+++

Kd: 464 nM

Phase 4

HJC0152√

SH5-07 (SH-5-07)√

APTSTAT3-9R√

Ochromycinone (STA-21)√

Phase 2

Napabucasin√

Phase 3

HO-3867√

Artesunate√

EXP1(a membrane glutathione
S-transferase)

Phase 4

注釈：
1.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
2.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

40

41

MAPK

阻害選択性
Inhibitor Name

MEK

MEK1

Cobimetinib (GDC-0973,
RG7420)

Cytokines, UV,Inflammatory

GPCR

LPS

IP3

Pan-Raf Inhibitors
Vemurafenib
Sorafenib
Dabrafenib
Selective Raf Inhibitors
GDC-0879 (B-Raf)
GW5074 (C-Raf)

A-Raf
Ras

PKC

B-Raf

MAP3K

Raf-1

MAP2K

MEK1,2

Neurofilament
Lin-1

MAPK

Vinexin

ATF1

MNK1

ERK1,2

MSK

RSK

CREB

GSK-3
IκBα

PI3Kγ

√

JNK Inhibitors
SP600125
JNK-IN-8JNK Inhibitor IX

ELK-1

ATF1/2/6
MEF2

JNK1,2,3

DUSP1

ETS-1

p38 MAPKα,β

Bcl-2
c-Jun
JNK
STAT4

NFK3

JunD

ATF2
HSF-1

MK2,3

BAD

ER81
eEF2K

p53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μCREB

CAMK Inhibitors
NH125
KN-93
KN-62

Raf

p53

Pan-p38 MAPK Inhibitors
SB203580
LY2228820
VX-702
Losmapimod
Selective p38 MAPK Inhibitors
BIRB 796 (p38α)
Skepinone-L (p38α)

JNK

詳細情報はP40に記載されています

MEK

C-Raf/Raf-1

B-Raf

A-raf

Other Targets

Clinical Phase+

IC50: 48 nM+

IC50: 31 nM

SRMS,ACK1,MAP4K5 (KHS1)

Phase 4+++

IC50: 6 nM++

IC50: 22 nM

VEGFR2/Flk1,mPDGFRβ,PDGFRβPhase 3

PLX-4720+++

IC50: 6.7 nM++

IC50: 13 nM

BRKDabrafenib (GSK2118436)+++

IC50: 6.3 nM++++ IC50: 0.7 nM

Sorafenib Tosylate

ATF4

p65

Akt-phosphorylation

Myricetin

Vemurafenib (PLX4032, RG7204)

MKK4,7Bid

p38 MAPKα,β14-3-3

SOS

Akt

√
√

Inhibitor Name

MLK1 DLKBax

MKK3,6

p53

c-Fos

c-Jun

Clinical Phase

阻害選択性
MLK3

MLK2

SAP-1
eIF4E

STAT3

Other Targets

TAK1

ASK1
TAO1,2

MNK

Histone H3

TCR

MEKK1-4

TAK1 MEKK1-4

Pan-MEK Inhibitors
Trametinib
U0126-EtOH
PD184352
Selective MEK Inhibitors
Selumetinib (MEK1)
BIX 02189 (MEK5)

Paxillin

ERK1,2

CDC40
TNFαRII

MEK5

Raf

CaMK

Ca2+

Honokiol

MEK2Phase 3

PD318088

Stress, LPS

CAMK Inhibitors
NH125
KN-93
KN-62

PLCβ

MEK1/2+++ IC50: 4.2 nM+++

IC50: 6 nM

Phase 4GDC-0879++++ IC50: 0.13 nM

RAF265 (CHIR-265)+

IC50: 3 nM-60 nM+

IC50: 34 nM

AZ 628+

IC50: 29 nM

NVP-BHG712+

IC50: 0.395 μM

SB590885

EphB4,c-Src,c-Abl+

IC50: 70 nM+++

IC50: 6 nM

GW5074++

IC50: 9 nM

TAK-632++++ IC50: 1.4 nM

CEP-32496+

Kd: 39 nM+++

IC50: 6.3 nM++++ IC50: 0.7 nM+++

IC50: 6 nM

Dabrafenib Mesylate
Regorafenib Monohydrate

Phase 2++++ Ki: 0.16 nM

ZM 336372
Sorafenib

VEGFR2++++ IC50: 2.5 nM++

IC50: 22 nM

mVEGFR2(Flk1),mVEGFR3,mPDGFRβ++IC50: 8.3 nM

Aurora B,PDGFRβ,FGFR3++

Kd: 14 nM

RET,PDGFRβ,LCK

IC50: 28 nM++++ IC50: 2.5 nM++

RAF709++++ IC50: 0.4 nM++++ IC50: 1 nM

Lifirafenib (BGB-283)+++

IC50: 7 nM++

IC50: 23 nM

CCT196969++

IC50: 0.01 μM+

IC50: 0.1 μM

BAW2881 (NVP-BAW2881)++

IC50: 24 nM

LY3009120+++

IC50: 4.3 nM+++

IC50: 5.8 nM

RO5126766 (CH5126766)+

IC50: 56 nM+++

IC50: 8.2 nM

Phase 4

RET,murine VEGFR2,KIT++++ IC50: 1 nM

EGFR,EGFR(T790M/L858R)

Phase 1

LCK,Src,V600E-BRAF
hVEGFR2,B-RAFV599E,c-Abl
Phase 1
Phase 1

MEK1

Encorafenib (LGX818)√

Phase 3

LXH254√Phase 1

PLX7904√

MLN2480√

Phase 2

阻害選択性
Inhibitor Name

MEK

MEK1/2+++ IC50: 14 nM

Selumetinib (AZD6244)
PD0325901

MEK1

MEK2
+

Clinical Phase
Phase 3

Kd: 530 nM

Phase 2++++ IC50: 0.92 nM

U0126-EtOH+

IC50: 0.07 μM++

IC50: 0.06 μM

PD184352 (CI-1040)++

IC50: 17 nM++

IC50: 17 nM

PD98059+

IC50: 2 μM

Phase 4++++ IC50: 1.8 nM

BIX 02189

Phase 2++++ IC50: 1.5 nM

Pimasertib (AS-703026)+

ERK5
Phase 2

IC50: 5 nM-2 μM

BIX 02188+++ IC50: 4.3 nM

TAK-733

Phase 1++++ IC50: 3.2 nM

AZD8330

ERK phosphorylation+++ IC50: 7 nM

Phase 1
Phase 3+++ IC50: 12 nM

SL-327+

IC50: 0.18 μM+

IC50: 0.22 μM

Refametinib (RDEA119,
Bay 86-9766)++IC50: 19 nM++

IC50: 47 nM

GDC-0623++++ IC50: 0.13 nM

BI-847325++

42

Other Targets++++ IC50: 0.33 nM

Trametinib (GSK1120212)

Binimetinib (MEK162,
ARRY-162, ARRY-438162)

MEK5

IC50: 25 nM

AP-1
Phase 2Phase 1+++ IC50: 4 nM

Aurora B (Xenopus laevis),Aurora C(Human),Aurora A (Human)

p38 MAPK
阻害選択性
Inhibitor Name
SB203580

p38 MAPK
+

p38α

p38β

Other Targets

Clinical Phase

PKB

IC50: 0.3 μM-0.5 μM

Phase 2

Doramapimod (BIRB 796)++++ IC50: 38 nM

SB202190 (FHPI)++

Ralimetinib (LY2228820)++++ IC50: 7 nM

VX-702+++

IC50: 4 nM-20 nM

PH-797804++

IC50: 26 nM+

IC50: 102 nM

Phase 2

VX-745+++

IC50: 10 nM+

IC50: 220 nM

Phase 2

TAK-715++++ IC50: 7.1 nM+

IC50: 0.20 μM

Phase 2

Pamapimod (R-1503, Ro4402257)+++

IC50: 0.014 μM+

IC50: 0.48 μM

SB239063++

IC50: 44 nM++

IC50: 44 nM

Losmapimod (GW856553X)++++ pKi: 8.1+++

pKi: 7.6

Skepinone-L++++ IC50: 5 nM

BMS-582949

Pexmetinib (ARRY-614)+++√

IC50: 50 nM++

IC50: 100 nM
Phase 2Phase 2Phase 2

IC50: 13 nM

Phase 3

Tie-2

Phase 143

Cytoskeletal Signaling

ERK
阻害選択性
Inhibitor Name

ERK1

ERK2

SCH772984+++

IC50: 4 nM++++ IC50: 1 nM

Magnolin++

IC50: 87 nM++

IC50: 16.5 nM

LY3214996+++

IC50: 5 nM+++

IC50: 5 nM

Pluripotin (SC1)++

Kd: 98 nM

ERK5

+++

Ulixertinib (BVD-523, VRT752271)+

Ki: 0.31 μM

NMDA

Phase 1F2R/CD14

IC50: 0.5 μM+

FN1Integrin
GPCR
FAK Inhibitors
PF-00562271
PF-562271
NVP-TAE226
PF-573228

SOS
Phase 2++++ IC50: 0.3 nM

Phase 1Gα12,13+

Pan-Raf Inhibitors
Vemurafenib
Sorafenib
Dabrafenib
Selective Raf Inhibitors
GDC-0879 (B-Raf)
GW5074 (C-Raf)Integrin
ClusteringCa2+

Ki: 0.14 μM

ERK5-IN-1

IC50: 162 nM

PI3K
RAP1

TOPK

PIP3

阻害選択性

RhoGEF

Calcineurin

Inhibitor Name++

IC50: 28 nM

OTS514 hydrochloride+++

IC50: 2.6 nM

ERK

MLCK

+++

IC50: 2.4 nM

CGP 57380++

IC50: 2.2 μM

MNK2Clinical Phase++++ IC50: 1 nM

Phase 2

CDK
Assembly

ERM

ACTN

Profilin
Focal
Adhesion
Assembly

Actin Polymerization
Stress Fiber

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

Rac1GEF

F-Actin2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

FGD1/3

GRLF1Cortactin
Cortactin

Cdc42

Dock180
IQGAP

APC

PIP2

+P
CFN

Actin
Polymerization

WAVE1

F-Actin

HSPC300

PXN
VCL

WAVE2

P

Cofilin

Focal Complex
Assembly

TMSB4

PFN

IRSp53ADF

F-Actin

NWASP

Nap125
PIR121
Abi2

LIMK
PI4P5K

Arp2/3APC Inhibitor
TAME

PAK

Asef

MLC
Cofilin

Y421 Y456 Y482

Cortactin

GIT1

PIP2

PFN

注釈：

CrkII

MBS

PI4P5K

Gβγ

Cas

Adherens
JunctionPIX

LIMK1,2

NHE1

mDia

FAK

ROCK Inhibitors
Y-27632
Thiazovivin
RKI-1447

ROCK1,2

p21

阻害選択性

Src

Rac

p27

MNK
eFT-508 (eFT508)

Pan-MEK Inhibitors
Trametinib
U0126-EtOH
PD184352
Selective MEK Inhibitors
Selumetinib (MEK1)
BIX 02189 (MEK5)MEK

ADF/Cofilin

Rho

MNK1

Src Inhibitors
Dasatinib
Saracatinib
Bosutinib
KX2-391

Ras

Raf

Vav

TOPK

OTS964

Inhibitor Name

Insulin, Growth Factor

IC50: 0.5 μM++++ IC50: <0.3 nM++

Pan-PI3K Inhibitors
BEZ235
GDC-0941
LY294002
Selective PI3K Inhibitors
HS-173 (p110α)
TGX-221 (p110β)
CZC24832 (p110γ)
CAL-101 (p110δ)F2+

FR 180204

Clinical Phase

Ki: <2 nM

DEL-22379++++ IC50: 1.1 nM

Other Targets

RasGAP

VX-11e

GDC-0994

ERK

Protein
Synthesis

Arp2/3eEF1Bα,γStabilizationof ActineEF1A

MyosinII

Akt

Bcr-Abl

FAK

HSP (e.g. HSP90)

詳細情報はP4に記載されています

詳細情報はP33に記載されています

詳細情報はP34に記載されています

詳細情報はP40に記載されています

Wnt/beta-catenin
阻害選択性

44

Inhibitor Name

Wnt/beta-catenin

XAV-939++++ IC50: 4 nM

ICG-001+

IC50: 3 μM

IWR-1-endo++

IC50: 180 nM

Wnt-C59 (C59)++++ IC50: 74 pM

IWP-2

+++

IWP-L6++++ EC50: 0.5 nM

iCRT3

+++

IC50: 8.2 nM

LF3+

IC50: 1.65 μM

Other Targets

Clinical Phase

IC50: 27 nM

45阻害選択性

阻害選択性

Inhibitor Name

Wnt/beta-catenin

PNU-74654++

Kd: 450 nM

KYA1797K+

IC50: 0.75 μM

PRI-724++

IC50: 150 nM

WIKI4

+++

IC50: 15 nM

LGK-974√

KY02111Isoquercitrin

Inhibitor Name

Microtubule Associated

Epothilone A++

EC0.01: 2 μM

Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium++

IC50: 2.4 μM

CW069

+

IC50: 75 μM

Combretastatin A4+++

Kd: 0.4 μM

CK-636++

IC50: 4 μM√

Docetaxel√√

ABT-751 (E7010)

√

IQ-1

√

Nocodazole√

Salinomycin (from Streptomyces albus)√

Cabazitaxel√

Phase 4

FH535√

Albendazole√

Phase 4Docetaxel Trihydrate√

Phase 4

PKC

TAI-1

√

INH6

√

阻害選択性

INH1

√

Vinorelbine Tartrate√

Triclabendazole√

Griseofulvin√

Inhibitor Name

PKC

PKCα

PKCβ
+++
IC50: 6 nM

Sotrastaurin++++
Ki: 0.95 nM++++
Ki: 0.64 nM

Staurosporine++++
IC50: 2 nM

Go 6983+++
IC50: 7 nM

Bisindolylmaleimide I (GF109203X)
Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

Dequalinium Chloride+
IC50: 7 μM-18 μM

Phase 2PPARγ,PPARδ++
IC50: 39 nM+
IC50: 25.01 μM

PKCγ

PKCδ

PKCθ

Other Targets

Clinical Phase
Phase 3++++
Ki: 3.2 nM++++
Ki: 1.8 nM++++
IC50: 5 nM+++
IC50: 20 nM++
IC50: 73 nM++++
IC50: 4 nM+++
IC50: 7 nM+++
IC50: 6 nM+++
IC50: 10 nM+++
IC50: 20 nM+++
IC50: 16 nM+++
IC50: 20 nM++++
IC50: 5 nM+++
IC50: 14 nM++
IC50: 27 nM++++
Ki: 0.22 nM
c-Fgr,phosphorylase kinase,S6 kinase

Phase 2++
IC50: 60 nM

Midostaurin (PKC412)++
IC50: 22 nM++
IC50: 30 nM++
IC50: 24 nM+
IC50: 330 nM++++
IC50: 2.3 nM+++
IC50: 6.2 nM

2-Methoxy-1,4-naphthoquinone+
IC50: 160 nM

PPK,KDR,c-Syk

Phase 1

Phase 2
Abl,Abl (E255K),Abl (T315I)

Phase 4Phase 3Integrin+++

IC50: 4.1 nM++

IC50: 20 nM

Phase 3

Cyclo(RGDyK)++

IC50: 20 nM

Phase 3

SB273005++++ IC50: 0.3 nM

RGD (Arg-Gly-Asp) Peptides√

Tirofiban√

Phase 4

Lifitegrast√

Phase 4

Tirofiban Hydrochloride√

Phase 2

ATN-161 (Ac-PHSCN-NH2)√

Phase 2

Cyclo (-RGDfK)√

Phase 3√
Sirtuin,Src,PI3Kγ

Phase 4√

Clinical Phase

A-205804

FLT3,JAK2√

Integrin

Cilengitide trifluoroacetate

Phase 3Phase 3

PAK

Kinesin

阻害選択性

阻害選択性
Inhibitor Name

KinesinClinical Phase

Ispinesib (SB-715992)+++

Ki app: 1.7 nM

Phase 2SB743921 HCl++++ IC50: 14.4 nM

Phase 2

AZ 3146+

IC50: ~35 nM

GSK923295++

Ki: 3.2 nM

Phase 1

BAY 1217389+++

IC50: 0.63 nM

Phase 1

MPI-0479605++

IC50: 1.8 nM

ARQ 621√

Phase 1

Microtubule AssociatedInhibitor Name

PAK

PAK1

PAK3

PAK2

IPA-3

+

IC50: 2.5 μM+

IC50: 2.5 μM

FRAX1036++

Ki: 72.4 nM++

Ki: 23.3 nM

FRAX486+++ IC50: 14 nM+++ IC50: 14 nM++

FRAX597++++ IC50: 13 nM++++ IC50: 8 nM+++ IC50: 19 nM++++ IC50: 13 nM

PF-3758309++++ IC50: 99 nM++++ Ki: 13.7 nM+++

KPT-9274√

IC50: 39 nM

IC50: 99 nM

PAK4

++

Ki: 72.4 nM+

Ki: 2.4 μM++

IC50: 33 nM+

IC50: 575 nM

IC50: 190 nM+++ Ki: 18.7 nM

PAK5

PAK6

+++ Ki: 18.1 nM+++ Ki: 17.1 nM

Other Targets

NAMPT

Dynamin
阻害選択性
Inhibitor Name

阻害選択性
Other Targets

Clinical Phase

DynaminDynasore++

IC50: ~15 μM

Mdivi-1+++

IC50: 1 μM-10 μM

Dyngo-4a++++ IC50: 0.38 μM

Inhibitor Name

Microtubule AssociatedPaclitaxel++++ IC50: 0.1 pM

Phase 4

Vincristine sulfate+

IC50: 32 μM

Phase 4

Patupilone (EPO906, Epothilone B)+++

EC0.01: 1.8 μM

Phase 3

注釈：

Lexibulin (CYT997)++++ IC50: 10 nM-100 nM

Phase 2

1.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。

46

Phase 3Phase 4

Inhibitor Name++
IC50: 0.052 μM+
IC50: 1.25 μM

Clinical Phase

阻害選択性

EGFR,PKA

Ruboxistaurin (LY333531 HCl)

Other Targets

Phase 2++
IC50: 24 nM+
IC50: 0.25 μM

Myricitrin

PKCη

++++
Ki: 2.1 nM+
IC50: 0.3 μM

Quercetin

PKCζ

+IC50: 110 nM++++
IC50: 4.7 nM+++
IC50: 7.9 nM

PKCε+IC50: 83 nM+
IC50: 0.36 μM

Go6976

Clinical Phase

Phase 1

Enzastaurin (LY317615)

Daphnetin

Other Targets

2.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

47

Cell Cycle
Pan-CDK Inhibitors
Palbociclib
Roscovitine
Dinaciclib
Selective CDK Inhibitors
XL413 (CDK7)
LDC000067 (CDK9)

阻害選択性
Inhibitor Name

Growth Factor
Withdrawal

Pan-Akt Inhibitors
MK-2206
Perifosine
GSK690693
Selective Akt Inhibitors
A-674563 (Akt1)
CCT128930 (Akt2)

Akt

TGF-β

FOXO1/3

Smad3
Smad4

c-Myc Inhibitor
10058-F4

ATM/
ATR

p27

CDK2

Cyclin D
G1- P HA

FOXO1 Bim
FasL
DBE

M-P

SE

Apoptosis

TRAIL

HAS

Pan-Aurora Kinase Inhibitors
VX-680Danusertib
ZM 447439
Selective Aurora Kinase Inhibitors
Alisertib (Aurora A)
Barasertib (Aurora B)
MK-5108 (Aurora A)

Cyclin E

S-

Abl Rb Suv39H1
E2F HDAC Rb
DP-1

E

OFF

E2F
DP-1

PH

AS

G2-P

CDK7

AurA
Bora

P P

Cyclin-A
P
P
CDK2
p21

cdc25A

Cyclin-A
CDK2
p27Kip1 P

Rad52

BRCA1

p53 Mdm2
Mdm4

ATM/ATR

c-Abl

Nuclear Export,
Ubiquitination

HIPK2

Rad51

++++
IC50: 6 nM

CDK6

CDK7

+++
IC50: 40 nM

CDK5

+++
IC50: 40 nM+
IC50: 300 nM+
IC50: 253 nM++
IC50: 175 nM

p53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μ
Mdm2 Antagonists
Nutlin-3
Nutlin-3a
YH239-EE
Mdm2 Activator
NSC 207895++
IC50: 60 nM++
IC50: 62 nM++++
IC50: 8 nM

Palbociclib (PD0332991)
Isethionate

UV

IR

Aurora Kinase

詳細情報はP17に記載されています++++
IC50: 9 nM+++
IC50: 15 nM++++
IC50: 2 nM+++
IC50: 10 nM

Phase 1++
IC50: 138 nM

Phase 2

GSK-3βPhase 1

Phase 4Phase 2+
IC50: 230 nM

BMS-265246++++
IC50: 9 nM

PHA-767491+
IC50: 250 nM+
IC50: 240 nM

Milciclib (PHA-848125)+
IC50: 398 nM++
IC50: 45 nM++
IC50: 160 nM

R547

++++
Ki: 2 nM++++
Ki: 3 nM++++
Ki: 1 nM

NU6027+
Ki: 2.5 μM+
Ki: 1.3 μM

P276-00++
IC50: 79 nM+
IC50: 224 nM+++
IC50: 10 nM

GSK-3β,MK2,PLK1++
IC50: 150 nM+
IC50: 265 nM

TrkA+
IC50: 2.87 μM+++
IC50: 20 nM

GSK-3βPhase 2+++
IC50: 13 nM

GSK-3α,GSK3β

Phase 1+++
IC50: 10 nM

Phase 3+
IC50: 17 μM

MSC2530818++++
IC50: 2.6 nM

Senexin A+
Kd: 0.83 μM

LY2857785++++
IC50: 0.246 μM IC50: 0.011 μM

LDC4297 (LDC044297)++++
IC50: 0.13 nM
ARK5,PDGFRβ,FGFR1+
IC50: 0.85μM+
IC50: 0.68μM

CDK19

+++
IC50: 0.016 μM++++
IC50: 9.82 nM++++
IC50: 3.87 nM+
IC50: 0.4μM

Phase 2

ATR,DNA-PK+
IC50: 396 nM++
IC50: 63 nM++++
IC50: 2 nM+
IC50: 26 μM+++
IC50: 10 nM+++
IC50: 34 nM+
IC50: 460 nM

GSK-3β,ERK2,c-Src++++
Kd: 18.6 nM++++
IC50: 3.2 nM+
IC50: 360 nM++
IC50: 100 nM

AT7519 HCl++
IC50: 210 nM++
IC50: 47 nM

Purvalanol A++++
IC50: 4 nM+++
IC50: 35 nM+
IC50: 850 nM

Ro-3306+++
Ki: 20 nM

SU9516+++
IC50: 40 nM+++
IC50: 22 nM++
IC50: 200 nM+++
IC50: 13 nM+++
IC50: <10 nM++
IC50: 170 nM

GSK-3βPhase 2++++
IC50: 4 nM
PKCδ,SGK,ERK++++
IC50: 3.4 nM++++
IC50: 3.4 nM

Pim1,CK2

Phase 2++
IC50: 44 nM+
IC50: 2.441 μM

ML167

++
IC50: 136 nM

TG003

+++
IC50: 15 nM

Ribociclib (LEE011)

CDK

Chk1

Akt1,PKA,GSK-3β++++
IC50: 6 nM

LDC000067

詳細情報はP10に記載されています

Other Targets Clinical Phase
Phase 2

XL413 (BMS-863233)

PD-1/PD-L1

CDK8

++
Ki: 46 nM

A-674563

Kenpaullone

DNA-PK Inhibitors
NU7441
NU7026
KU-0060648
PIK-75

Cdc+++
IC50: 21 nM

K03861

TRF2 POT1

CDK

Aurora A,Aurora B,
VEGFR2+++
IC50: 10 nM++++
IC50: 5 nM

THZ1 2HCl

Critically Short
Telomeres

CLK++
IC50: 0.16 μM

ON123300

FANCD2

CDK9+++
IC50: 20 nM

BS-181 HCl

NU2058

DNA-PK

Bcr-Abl Inhibitors
Imatinib
Ponatinib
Nilotinib
Bafetinib
Dasatinib+++
IC50: 16 nM++
IC50: 58 nM

Abemaciclib

TopoII

cdc25
Chk1

AZD5438

14-3-3

p21Cip1

Chk2++++
IC50: 3 nM

CDK4Atuveciclib (BAY-1143572)

Nuclear Exclusion

p53

Pan-PLK Inhibitor
BI 2536
Selective PLK Inhibitors
Volasertib (PLK1)
Rigosertib (PLK1)
GSK461364 (PLK1)

Cyclin-H
CDK7
P

P

P

GADD45
PLK1

Rb

Raf1 Wee1

HASE

JNJ-7706621++++
IC50: 9 nM

CDK3

abemaciclib mesylate(LY2835219)

E2F
Rb

E

E2F/DP Target Genes:
Cyclin E/A, E2F-1/2/3,
cdc2, c-Myc, p107,
ON RanGAP, TK, DHFR,
PCNA, H2A, etc.

Cyclin B
cdc2

Wee1

Pan-Chk Inhibitor
AZD7762
Selective Chk Inhibitors
LY2603618 (Chk1)
MK-8776 (Chk1)
CHIR-124 (Chk1)

Chk1/2

CDK4/6

Flavopiridol HCl+++
IC50: 40 nM

PHA-793887

DNA Damage

p21Cip1
Pan-HDAC Inhibitors
Vorinostat
Entinostat
Panobinostat
Selective HDAC Inhibitors
RGFP966 (HDAC3)
Nexturastat A (HDAC6)
PCI-34051 (HDAC8)

CDK2

+++
IC50: 40 nM

MK-8776 (SCH 900776)

p53

Kip1

cdc25A

Pan-GSK-3 Inhibitors
CHIR-99021
SB216763
CHIR-98014
Selective GSK-3 Inhibitors
TWS119 (GSK-3β)
Tideglusib (GSK-3β)

Dual ATM/ATR Inhibitors
Wortmannin
CGK 733
Selective ATM/ATR Inhibitors
KU-55933 (ATM)VE-821 (ATR)

Myc

Myc

GSK-3βDNA
RepairGrowth Factor
Receptor Activation

Pan-TGF-beta/Smad Inhibitors
LDN-193189
LDN-212854
K02288
Selective TGF-beta/Smad Inhibitors
DMH1 (ALK2)
SB431542 (ALK5)

CDK1

Phase 3√

WogoninN-acetyltransferase

√

阻害選択性
Inhibitor Name

CDK1

CDK2

CDK3

+
IC50: 0.65 μM

SNS-032 (BMS-387032)++
IC50: 0.16 μM+++
IC50: 38 nM+
IC50: 340 nM++++
IC50: 1 nM++++
IC50: 3 nM++++
IC50: 1 nM

Flavopiridol (Alvocidib)+++
IC50: 30 nM+++
IC50: 40 nM

AT7519++
IC50: 210 nM++
IC50: 47 nM+++
IC50: 20-40 nM+
IC50: 360 nM++
IC50: 100 nM

CDK6

CDK7

CDK9

CLK

CDK

Cdc

CDK8

Other Targets Clinical Phase+++
IC50: 15 nM+
IC50: 0.7 μM

Dinaciclib (SCH727965)

48

CDK5

++++
IC50: 9 nM

Palbociclib (PD-0332991) HCl

Roscovitine (Seliciclib,CYC202)

CDK4+
IC50: 0.65 μM++
IC50: 62 nM++
IC50: 60 nM+++
IC50: 13 nM

Phase 4++
IC50: 170 nM+
IC50: 875 nM++++
IC50: 4 nM

阻害選択性
ERK2

Phase 2

GSK-3αPhase 1

Chk1+++

IC50: 5 nM

Rabusertib (LY2603618)++

IC50: 7 nM

Phase 2

MK-8776 (SCH 900776)+++

IC50: 3 nM

Phase 2CHIR-124++++ IC50: 0.3 nM

Phase 3+++
IC50: 20 nM
GSK-3βInhibitor NameAZD7762++++
IC50: 4 nM+++
IC50: <10 nM

Chk
Chk2
++

Other Targets

IC50: <10 nM

Clinical Phase
Phase 1
Phase 2

CDK2

Phase 2

FLT3,PDGFR,GSK-3

49

Rho

阻害選択性
Inhibitor Name

Chk1

PF-477736++++ Ki: 0.49 nM

GDC-0575 (ARRY-575, RG7741)+++

IC50: 1.2 nM

CCT245737+++

IC50: 1.4 nM

SAR-020106+

IC50: 13.3 nM

Prexasertib HCl (LY2606368)++++ Ki: 0.9 nM

Chk2

Other Targets

Clinical Phase

Ki: 47 nM

VEGFR2,Fms,YES

Phase 1+

Phase 1

Chk2 Inhibitor II (BML-277)+

IC50: 15 nM++

IC50: 8 nM

RSKPhase 2ROCK
阻害選択性
Inhibitor Name

ROCK

ROCK1

Y-27632 2HCl++Thiazovivin

+

ROCK2

Ki: 140 nM++

GSK429286A
RKI-1447++

Clinical Phase

Ki: 300 nM

IC50: ~0.5 μM

Fasudil (HA-1077) HCl

GSK180736A (GSK180736)

Other Targets

PKA,PKG,PKC

Ki: 330 nM+++

IC50: 14 nM++

IC50: 63 nM+++

IC50: 14.5 nM+++

IC50: 6.2 nM
GRK2,PKA,GRK5

IC50: 100 nM

Hydroxyfasudil (HA-1100) HCl+

Y-39983 HCl++++ IC50: 3.6 nM

Netarsudil (AR-13324) 2HCl++++ Ki: 2 nM

Phase 3+

IC50: 0.73 μM

IC50: 0.72 μM

norepinephrine transporter (NET)Phase 3

MSK1,RSK1++++ IC50: 1.6 nM++++ IC50: 4 nM

Ripasudil (K-115) hydrochloride dihydrate

++

+++

IC50: 19 nM

Phase 4++

IC50: 60 nM

Phase 2KD025 (SLx-2119)
AT13148+++

Phase 1

阻害選択性
PLK1

BI 2536++++ IC50: 0.83 nM

Volasertib (BI 6727)++++ IC50: 0.87 nM

Rigosertib (ON-01910)+

IC50: 9 nM

GSK461364+++

Ki: 2.2 nM

MLN0905+++

IC50: 2 nM

Ro3280++IC50: 3 nM

PLK2
++

+

IC50: 3.5 nM

PLK3
+

PLK4

NMS-P937 (NMS1286937)+++

HMN-214√

Clinical Phase
Phase 2PDGFR,Bcr-Abl,Flt1

EHop-016+++

IC50: 1.1 μM

ZCL278+

Kd: 11.4 μM

MBQ-167+++

IC50: 78 nM

KRpep-2d++++ IC50: 1.6 nM

ARS-853 (ARS853)++

IC50: 2.5 μM

Salirasib++

Ki: 2.6 μM

ML141

+++

IC50: 200 nM

EHT 1864 2HCl++++ Kd: 40 nM

Zoledronic Acid√

Phase 4

Azathioprine√

Phase 4

CCG-1423√

K-Ras(G12C) inhibitor 9√

K-Ras(G12C) inhibitor 6√

K-Ras(G12C) inhibitor 12

√

6H05

√

Phase 2

DYRK
Inhibitor Name

DYRK

DYRK1

AZ191

++++ IC50: 17 nM

Harmine hydrochloride

+++

DYRK2

IC50: 33 nM++

IC50: 1.9 μM

Other Targets

MNB

√

c-Myc
阻害選択性

Phase 3

Inhibitor Namec-Myc

Phase 310074-G5+++

Phase 110058-F4√

Kd: 2.8 μM

注釈：++++++ IC50: 200 pM

Other Targets

IC50: 9.0 nM

IC50: 260 nM

CFI-400945
SBE 13 HCl

Clinical Phase

IC50: 50 μM

ID-8

PLK
Inhibitor Name

Rho
+

阻害選択性

PKA,p70S6K,Akt1++++ IC50: 4 nM

IC50: 6 nM

Inhibitor Name
NSC 23766

PKA

GSK269962A HCl

IC50: 51 nM

阻害選択性

IC50: 2.8 nM

TrkA,TrkB,Tie-2

Phase 2

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

IC50: 2 nM

Phase 1

APC
阻害選択性
Inhibitor Name

APC

TAME

√

Wee1
阻害選択性
Inhibitor Name

Wee1

Adavosertib (MK-1775)+++

IC50: 5.2 nM

PD0166285++

IC50: 24 nM

50

Other Targets

Clinical Phase
Phase 2

Myt1,Chk1

51

TGF-beta/SmadDNA Damage
Pan-TGF-beta/Smad Inhibitors
LDN-193189
LDN-212854
K02288
Selective TGF-beta/Smad Inhibitors
DMH1 (ALK2)
SB431542 (ALK5)

TGFβ

CDC42

ROCK

Smad7

PAK Inhibitors
IPA-3
PF-3758309

PAK
LIMK

PKC

Actin Polymerization
Stress Fibers

Cell Adhesion

MEKs
Smad4

MAPK
Pathway
Smad3/4

Apoptosis
CBP

Smad2

SBE

P300 Smad4

PKC 詳細情報はP46に記載されています

Bcr-Abl 詳細情報はP33に記載されています

阻害選択性
ALK1

ALK2

ALK3

ALK4

SB431542

TGFβRI/ALK5+

IC50: 94 nM

Galunisertib (LY2157299)++

IC50: 56 nM

LY2109761++

Ki: 38 nM

SB525334+++ IC50: 14.3 nM++++ IC50: 5 nM

LDN-193189+

IC50: 129 nM+++++ IC50: 18 nM

LY364947++

RepSox++++ IC50: 4 nM++++ IC50: 5 nM++++ IC50: 1.8 nM ++++ IC50: 1.1 nM

TGFβRII

TGF-β Smad3

Other
Targets

Clinical Phase

Phase 3
+ Ki: 300 nM

IC50: 59 nM++ IC50: 34.4 nM

Vactosertib (TEW-7197)

RIPK2,CK1δ,
MLK-7K+ IC50: 0.4 μM++++ IC50: 2.4 nM ++++ IC50: 1.3 nM
+

CDK

Wee1

Cell Cycle

PARP

Sirtuin

Pan-Topoisomerase Inhibitor
Moxifloxacin
Selective Topoisomerase Inhibitors
Camptothecin (Topo I)
Topotecan (Topo I)
Doxorubicin (Topo II)
Etoposide (Topo II)

詳細情報はP11に記載されています

DNA-PK

詳細情報はP6に記載されていますTopoisomerase

IC50: 48 nM
Phase 1+++ IC50: 11 nM

IC50: 2133 nM +IC50: 9276 nM

IC50: 107.9 nM

Pirfenidone√

Phase 4

Alantolactone√

SIS3 HCl√

Hesperetin

注釈：

Topo I

Camptothecin++

Topotecan HCl++++ IC50: 2 nM

√

STAT3

Histamine
receptor

Topo II

Other Targets

Clinical Phase
Phase 2

IC50: 0.68 μM

Phase 4++++++Topo IV

IC50: 3.3 ng/mL

Multicellular spheroids

Phase 4Phase 4

Ki: 20 nM++

HIV-1,Aminopeptidase N

IC50: 5 μM

Phase 2

Flumequine+

Doxorubicin (Adriamycin) HCl√

Phase 4

Etoposide√

Phase 4

Epirubicin HCl++ IC50: 85.8 nM +Topoisomerase

Betulinic acid+++ IC50: 32 nM

LDN-212854

AuroraKinase

詳細情報はP5に記載されています

Idarubicin HCl++++ IC50: 6.4 nM+++ IC50: 13 nM
IC50: 46 nM

CDC25

ATM/ATR

Daunorubicin HCl

++

++

PLK

HDAC

Inhibitor Name+++ IC50: 30 nM

SD-208

ML347

Chromatin
Remodeling

阻害選択性+++ IC50: 24 nM

LDN-214117

DMH1

ALK6

IC50: 47 nM

GW788388

K02288

Pan-PARP Inhibitors
Olaparib
Veliparib
Selective PARP Inhibitors
AG-14361 (PARP1)
UPF 1069 (PARP2)
ME0328 (PARP3)

TLK1/2+++ IC50: 30 nM

SB505124

LDN-193189 2HCl

Pan-Chk Inhibitor
AZD7762
Selective Chk Inhibitors
LY2603618 (Chk1)
MK-8776 (Chk1)
CHIR-124 (Chk1)

詳細情報はP8に記載されています

TGF-beta/Smad
Inhibitor Name

p53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μ

詳細情報はP7に記載されていますROCK 詳細情報はP50に記載されていますTopoisomerase

Chk1

PARP

Pan-TGF-beta/Smad Inhibitors
LDN-193189
LDN-212854
K02288
Selective TGF-beta/Smad Inhibitors
DMH1 (ALK2)
SB431542 (ALK5)ATMDNA Repair
Chk2

Smad2/4

ATR

H2AX

Mdm2

ERK1/2

Transcription

Tumor
Angiogenesis
Suppression Cell Growth

Pan-MEK Inhibitors
Trametinib
U0126-EtOH
PD184352
Selective MEK Inhibitors
Selumetinib (MEK1)
BIX 02189 (MEK5)

c-Abl

p53

Apoptosis

Ras

Smad3

PI3K/Akt
Pathwayc-Abl
Bcr-Abl Inhibitors
Imatinib
Ponatinib
Nilotinib
Bafetinib
Dasatinib

Smad6
Smad2

DNA-PK Inhibitors
NU7441
NU7026
KU-0060648
PIK-75

DNA-PK

Replication Stress

BRCA1

ATM

JAK

Rho Family Inhibitors
Zoledronic Acid
NSC 23766
EHop-016
ZCL278ROCK Inhibitors
Y-27632
Thiazovivin
RKI-1447

Alkylating Agents

Double-strand Breaks

Dual ATM/ATR Inhibitors
Wortmannin
CGK 733
Selective ATM/ATR Inhibitors
KU-55933 (ATM)VE-821 (ATR)

IC50: 15 μM

Phase 4√

Mitoxantrone 2HCl√

Phase 4

Moxifloxacin HCl√

Phase 4

Irinotecan HCl Trihydrate

√

SN-38

√

Phase 4Phase 2

Amonafide√

Phase 3Teniposide√

Phase 4Gatifloxacin√

Phase 4

1.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
2.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

5253

阻害選択性Inhibitor Name

Topoisomerase

Topo I

Topo II

Dexrazoxane HCl (ICRF-187, ADR-529)√

Genistein√

Levofloxacin√

Pirarubicin√

Topo IV

Other Targets

Clinical Phase
Phase 3

EGFR

Phase 4√√

Novobiocin Sodium√

Enoxacin√

Ofloxacin√

Nalidixic acid

Hedgehog Inhibitor
Vismodegib

Phase 4Smo

PTC

Frizzled√

Phase 4

IDO1

Clinafloxacin

Phase 2√√

Voreloxin (SNS-595) hydrochloride√

Pefloxacin Mesylate Dihydrate√

Phase 3

Telomerase
阻害選択性
Inhibitor Name

Telomerase

BIBR 1532+++

IC50: 100 nM

Costunolide++

IC50: 65 μM

RHPS 4 methosulfate√

GSK-3β

Wnt/beta-catenin
Inhibitors
XAV-939
ICG-001
LGK-974
IWP-2
Wnt-C59

Other Targets

FPTaseAxin

SUFU(cAMP)
PKA

APC

Axin

GSK-3β β-cat

Ub

Ub Ub

Ub

β-cat

Rho

FGF
gp130

FGFR

TGFβRⅠ,TGFβRⅡ
STAT3

Gamma-secretase
Inhibitors
DAPT
RO4929097
Semagacestat
MK-0752
Avagacestat

Rac
Ca2+

P

PKC

MAPK

Ronin
Cdx2 Others
Caspase-3

JNK

Proteasome

Gli

α
β γ
GTP
α
GTP
PLC

DSH

GRK

GTP

Intracellular
VesiclePan-GSK-3 Inhibitors
CHIR-99021
SB216763
CHIR-98014
Selective GSK-3 Inhibitors
TWS119 (GSK-3β)
Tideglusib (GSK-3β)

GSK-3β

αi

PI3K

Akt

Phase 1

√

β γ

P

CKI

P

LIF

LIFR

γ-Secretase

P

Phase 2

Levofloxacin hydrate

TGFβ

BMP

ADAM17

Sanpodo S2

Tra
ns
loc
ati
on

Beta-Lapachone

Pan-TGF-beta/Smad Inhibitors
LDN-193189
LDN-212854
K02288
Selective TGF-beta/Smad Inhibitors
DMH1 (ALK2)
SB431542 (ALK5)

Wnt

P

√

Dll1,3,4/Jagged1,2

Hedgehog√

Ellagic acid(S)-10-Hydroxycamptothecin

Wnt/beta-catenin
Inhibitors
XAV-939
ICG-001
LGK-974
IWP-2
Wnt-C59

Smoothened Antagonists
Cyclopamine
LDE225
LY2940680
BMS-833923
Smoothened Agonist
Purmorphamine

Phase 4Phase 4

Ciprofloxacin
Marbofloxacin

Stem Cells & Wnt

Gata6

β-cat
β-cat
Gli

SHARP
HDAC
CtBp
SMRT
Hes1
Hey1

API

TCF/LEF NFAT

Nicd Smad1

Gene ExpressionP

CSL Smad4

P

Nicd
Herp2
Hey

CSL

P300 E(Spl)

Mam

Hes1

TAK2

P

Hes1 STAT3
STAT3

P

P

STAT3

Hes1
Hey

Pan-STAT Inhibitor
SH-4-54
Selective STAT Inhibitors
Fludarabine (STAT1)
S3I-201 (STAT3)
Cryptotanshinone (STAT3)

P

Smad1
P

Gfap

Smad4

P

Idl

MTH1
阻害選択性
Inhibitor Name

MTH1

TH287

++++ IC50: 0.8 nM

TH588

+++

IC50: 5 nM(S)-crizotinib++

IC50: 72 nM

注釈：

GSK-3

JAK

STAT

TGF-beta/Smad

Wnt/beta-cateninROCK

詳細情報はP4に記載されています

詳細情報はP9に記載されています

詳細情報はP41に記載されています

詳細情報はP52に記載されています

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

詳細情報はP45に記載されています

詳細情報はP50に記載されています

Gamma-secretase
阻害選択性
Inhibitor Nameγ secretase

DAPT (GSI-IX)
RO4929097+++

Semagacestat (LY450139)++

Avagacestat (BMS-708163)++++ IC50: 0.27 nM

Dibenzazepine (YO-01027)+++

LY411575++++ IC50: 0.078 nM

IC50: 2.6 nM

L-685,458

Notch

IC50: 10.9 nM

Clinical Phase
Phase 4+++

IC50: 5 nM++

IC50: 14.1 nM+++

IC50: 2.9 nM

Aβ40

Phase 2Phase 3Phase 2++++ IC50: 0.39 nM+++

Other Targets

IC50: 20 nM

IC50: 4 nM

IMR-1

54

Aβ
+

IC50: 26 μM

Ki: 17 nM

55

阻害選択性Inhibitor Nameγ secretase

Aβ

Notch

FLI-06+Crenigacestat (LY3039478)++++ IC50: ~1 nM

Nirogacestat (PF-03084014, PF-3084014)++

Other Targets

Ubiquitin

EC50: 2.3 μM

Phase 2Aβ√E2

E1 Activating Inhibitor
PYR-41

Phase 2=Hedgehog/Smoothened

DUB Inhibitors
PR-619
IU1
P5091
ML323
Degrasyn

阻害選択性
Inhibitor Name

Hedgehog+++

Vismodegib (GDC-0449)

Smoothened

GLI

Other Targets

Clinical Phase
Phase 4

IC50: 3 nM
IC50: 46 nM

Cyclopamine++

Sonidegib (Erismodegib, NVP-LDE225)++++ IC50: 1.3 nM

PF-5274857+++

Phase 3

IC50: 5.8 nM

GANT61+

IC50: 5 μM

Glasdegib (PF-04449913)++

Taladegib (LY2940680)√

BMS-833923

Phase 2Phase 2√

Jervine√

HPI-4 (Ciliobrevin A)√

Shh

MK-4101

CDK–cyclin A

S

G1

Proteasome

√

Ub Ub

NF-κB Inhibitors
QNZ
Sodium 4-Aminosalicylate
JSH-23SC75741

ATPIκB Kinase
Cellular StressProteasome

CDK–cyclin D

ARF
Gene
Expression

p53
Mdm2

Proteasome
Ub
Ub
Ub

CDC25A, CDC25C
KIP1

StressApoptosis

Mdm2 Antagonists
Nutlin-3
Nutlin-3a
YH239-EE
Mdm2 Activator
NSC 207895

CDK–cyclin E

p53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μ

p53
p53

Apoptosis

P

IκB NF-κB

Ub
Ub
Ub

Proteasome Inhibition

Pro-survival
Pathway

P

IκB
Gene
Expression

NF-κB

SenescenceProteasome Inhibition

Casein Kinase

Pan-IκB/IKK Inhibitors
IKK-16
Bardoxolone Methyl
Selective IκB/IKK Inhibitors
TPCA-1 (IKK-2)
IMD 0354 (IKK-2)

NH
C= O

Cellular Pathways Associated with the Proteasome

CDK–cyclin B
CDK–cyclin A
G0

M
G2

S

DUBs
Ub Ub
Ub Ub

ADP+Pi

DUB Inhibitors
PR-619
IU1
P5091
ML323
DegrasynDUBs

S

26S Proteasome

DUBs

CDC25C

CDC25B

Phase 3

DUBs

Proteasome
Proteasome
WAF1

IC50: 5 nM

Ub

Ub

Ub

Ub RP

Proteasome++++ Kd: 1.2 nM

SANT-1Ub Ub Ub Ub Ub

Pan-Proteasome Inhibitor
Oprozomib
Selective Proteasome Inhibitors
Bortezomib (20S proteasome)
Carfilzomib (20S proteasome)
MLN9708 (20S proteasome)
ONX-0914 (LMP7)

S
C=O

HECT

S
C=O

S

E2

HECT-type E3

Ub

AMP+PPiO
Ub C S
E1

RING Finger

E2 Conjugating Inhibitors
NSC697923
BAY 11-7082

S
C=O

ATP

Phase 1√E3 Ligase Activators(-)-Parthenolide
NSC 207895
E3 Ligase Antagonists
JNJ-26854165
Thalidomide
Nutlin-3

RING-type E3

Phase 2

IC50: 6.2 nM

MK-0752
NGP 555

Clinical Phase

Proteasome InhibitionIκB NF-κB

阻害選択性
Inhibitor Name

CK1

CK2

Other Targets++++ IC50: 1 nM

TBB+

Ki: 0.4 μM

CK1

Ellagic Acid hydrate+++

IC50: 0.04 μM

Lyn,PKA

D 4476++

Clinical Phase
Phase 2

Silmitasertib (CX-4945)

IC50: 200 nM

阻害選択性
Inhibitor Name

ALK5

Hippo pathway
YAP/TEAD interaction

XMU-MP-1
YAP-TEAD Inhibitor 1 (Peptide 17)

Proteasome

MST1
++

IC50: 71.1 nM

MST2
+++

Other Targets

Clinical Phase

IC50: 38.1 nM++++ IC50: 25 nM

Verteporfin√

Super-TDU

√

注釈：

VDA

Phase 420S proteasome

Bortezomib (PS-341)++++ Ki: 0.6 nM

MG-132+

Carfilzomib (PR-171)

阻害選択性
Inhibitor Name

Proteasome+++

Clinical Phase
Phase 4

IC50: 100 nM
Phase 4

IC50: 5 nM
IC50: 3.4 nM

Ixazomib Citrate (MLN9708)+++

Ixazomib (MLN2238)++++ IC50: 3.4 nM

ONX-0914 (PR-957)++

IC50: ~10 nM

Oprozomib (ONX 0912)++

IC50: 36 nM

Phase 2

Delanzomib (CEP-18770)+++

IC50: 3.8 nM

Phase 2

Celastrol+

IC50: 2.5 μM

PI-1840++

IC50: 27 nM

Epoxomicin

√

VR23

Phase 3++++ IC50: 1 nM

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

DUB
阻害選択性
Inhibitor Name

USP/UBP

PR-619++EC50: 7.20 μM

P5091 (P005091)++

IC50: 4.3 μM

TCID

56

DUB

UCH
+++

EC50: 2.95 μM+++

IC50: 0.6 μM

Other Targets

Clinical PhaseJOSD2,SENP6 core,DEN1

Phase 157

阻害選択性Inhibitor NameDUB

USP/UBPUCH

LDN-57444

Clinical Phase

Neuronal Signaling++++ IC50: 0.88 μM

IU1

++

P22077

ML323++++ IC50: 76 nM

CB1/2

mGLuR

IC50: 8.6 μM

b-AP15

+++

NMDAR

GABA

P2X

ACh

GABAR

AChR

IC50: 2.1 μM
Bcr-Abl√GluR Agonists
LY404039
ADX-47273
VU 0364439
GluR Antagonists
CTEP
MPEP
Latrepirdine

E3 Ligase
E3 Ligase

CRBN

Other Targets

Na+

G-protein
GPCR
Pathway

阻害選択性
Inhibitor Name

AMPAK

ATP

Phase 2

IC50: ~10 μM+

Glutamute

Glutamate

IC50: 4.7 μM+

VLX1570

Degrasyn (WP1130)

Other Targets

Clinical Phase

Ca2+
MEK

Cannabinoid Receptor
Antagonists
RimonabantOtenabant
AM251
Cannabinoid Receptor
Agonists
AM1241
BML-190
GW842166X

ERK
MAPK
Pathway

Cl

CaM

-

AChR Antagonists
PNU-120596
Atropine
Aclidinium
AChR Agonists
Bethanechol
Arecoline
Decamethonium

GABA Receptor Antagonists(+)-Bicuculline
Ginkgolide A
Flumazenil
GABA Receptor Agonists
Gabapentin(R)-baclofen
Etomidate

CaMK
nNOS

IC50: 180 nM

Nutlin-3+++

JNJ-26854165 (Serdemetan)√

p53

Phase 1

Thalidomide√

TNF-alphaPhase 4

TAME√

Tenovin-1√

RITA (NSC 652287)√

p53

Avadomide(CC-122)√

COX

Gamma-secretase

詳細情報はP18に記載されていますp53

詳細情報はP55に記載されています

Phase 2Phase 2

Histamine Receptor

詳細情報はP19に記載されていますp97

Beta Amyloid

阻害選択性
Inhibitor Name

p97

Other Targets

NMS-873++++ IC50: 30 nM

DBeQ

+++

IC50: 1.5 μM

MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)++

IC50: 1.7 μM

Clinical Phase

Inhibitor Name

Syk,SrcPhase 2E1 Activating
阻害選択性
Inhibitor Name

阻害選択性
Beta Amyloid

DAPT (GSI-IX)++

IC50: 20 nM

RO4929097+++

IC50: 14 nM

MK-0752+++

IC50: 5 nM

Avagacestat (BMS-708163)++++ IC50: 0.27 nM

LY2811376+

Tabersonine hydrochloride√

EUK 134√

Other Targets

Clinical Phase
Phase 4γ secretase,γ secretase(ICN)

Phase 2Phase 2Phase 2

EC50: ~300 nM

BACE1

Phase 1E1 Activating

PYR-41+++

IC50: <10 μM

5-HT Receptor
阻害選択性

E2 conjugating

Inhibitor Name

阻害選択性
E2 conjugating

Other Targets

BAY 11-7082

Inhibitor Name√IκBα phosphorylation

NSC697923√

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

5-HT

5-HT1

5-HT2

Ketanserin+++ Ki: 2.5 nM

RS-127445++++ pIC50: 10.4

5-HT6

Other Targets

Clinical Phase
Phase 4Phase 4++

Ki: 6.6 nM+

α2c-adrenergic receptor,
D2 receptor,D3 receptor

Phase 4++

Ki: 19 nM

SERT

Phase 4

Ki: 3.98 nM

dopamine D2 receptor

Phase 3

pIC50: 5.5

α1D-adrenoceptor,Dopamine
D2 receptor,α2C-adrenoceptor++

Ki: 14.9 nM++++ Ki: 0.17 nM

Vortioxetine (Lu AA21004) HBr++

Ki: 15 nM++++ pKi: 9.6+++ IC50: 0.95 nM

Blonanserin+++ Ki: 3.7 nM++++

BMY 7378 Dihydrochloride

pIC50: 5.9

PRX-08066 Maleic acid+

Ki: 206 nM+++ IC50: 3.4 nM

SB742457

Phase 2Phase 2++++ pKi: 9.63

SB269970 HCl++

BRL-15572(dihydrochloride)

58

5-HT5

α2B-adrenergic receptor,
D3 receptor,H1 receptor

Risperidone

Desvenlafaxine

5-HT7+++ pKi: 8.84++++ pKi: 9.75

WAY-100635 Maleate

5-HT4++++ pKi: 9.94+++ pKi: 8.4

Asenapine maleate

5-HT3

+

Ki: 40.2 nM

pKi: 5.2+

pKi: 6.6+

pKi: 5.9++

pKi: 8.3+

pKi: 6.3
Norepinephrine (NE)

Phase 459

阻害選択性

阻害選択性

Inhibitor Name

5-HT

Sertraline HCl++ Ki: 13 nM

Lamotrigine+

Escitalopram Oxalate+++ Ki: 0.89 nM

5-HT1

5-HT2

5-HT3

5-HT4

Other Targets

Clinical Phase

Inhibitor Name

Phase 4

IEM 1754 2HBr

Phase 4MPEP

Phase 4

Riluzole++

Ki: 6.6 nM+

IC50: 235 nM

NMDA receptor

AMPA receptor+

mGluR5GluR

D4 receptor (human),D2 receptor (Human),D2 receptor (bovine)

Phase 4++

Serotonin receptor,Norepinephrine receptor,
Sigma 1 receptor

Phase 4

D2 receptor

Phase 4

α7 nAChR

Phase 4

Clinical Phase

Sodium channel,Glutamate release

Phase 45-HT,Histamine receptor

Phase 3

IC50: 36 nM√√

Evans Blue

Other Targets

IC50: 6 μM

Latrepirdine 2HCl++++ IC50: 0.33 nM

SB 271046 hydrochloride

vesicular glutamate uptake√+++ pKi: 8.92

Amitriptyline HCl
Palonosetron++ IC50: 7.31 nM++++ Ki: 0.17 nM++ Ki: 6.4 nM

lurasidone++++ Ki: 0.5 nM

Tropisetron++++ Ki: 0.5 nM+++++ Ki: 2.9 nM

Perospirone hydrochloride

Ki: 5.3 nM++++ Ki: 0.091 nM+++ Ki: 1 nM

Flibanserin
Sarpogrelate hydrochloride+

D4 receptor

Ki: 49 nM++++ Kd: 0.2 nM+++ IC50: 1.8 nM

Ondansetron Hydrochloride
Dihydrate+

Cyproheptadine hydrochloride
sesquihydrate+++ IC50: 0.6 nM

Pimavanserin+++ pIC50: 8.7+

IC50: 810 nM

Norepinephrine (NE)VUF 10166

Asenapine maleate

Phase 4

Nebivolol HCl

Phase 3

BMY 7378 Dihydrochloride

Phase 3

Propranolol HCl

Phase 1

Norepinephrine (NE) transporter,
DA transporter√

Clozapine√

Fluoxetine HCl√

Latrepirdine 2HCl√

Agomelatine

D2 receptor

Histamine receptor,GluR√+++

pKi: 6.54

Naftopidil+++

Ki: 1.2 nM

Naftopidil DiHCl++

IC50: 0.2 μM

pIC50: 5.1++

IC50: 12 nM

Phase 4
5-HT1A,Dopamine D2 receptor,
5-HT1C
Phase 4Phase 4
5-HT1A
Phase 4

Betaxolol HCl+

IC50: 6 μM

Phase 3+

Kd: 0.25 μM++

Ki: 12 nM

Piribedil++

pKi: 7.1

Phase 4

Tamsulosin hydrochloride++++ Ki: 0.18 nM

Phase 4

ICI-118551 Hydrochloride

Phase 4

Levobetaxolol HCl

Phase 3Doxazosin Mesylate√

Phase 2Phase 4

Alfuzosin HCl√

Phase 4Phase 4

Silodosin√

Phase 4Phase 4

Phentolamine Mesylate√

Phase 3Phase 4

Prazosin HCl√

Phase 4

Bisoprolol fumarate

Phase 4

Atenolol√

Dapoxetine HCl√

Ziprasidone HCl√

Iloperidone√

Phase 4

Terazosin HCl Dihydrate

Mirtazapine√

Phase 4Metoprolol Tartrate

Phase 4

Carvedilol√

IC50: 0.8 nM+

Phase 4Phase 4

Paroxetine HCl

Granisetron HCl+++

Clinical Phase

Ki: 1.97 nM√

Dopamine receptor

Other Targets
5-HT2C,5-HT2A,5-HT7+++

Venlafaxine HCl

AChR

β-adrenergic receptor

Timolol Maleate

Ki: 249 nM

Olanzapine

α-adrenergic receptor++++ pKi: 8.9

Rauwolscine hydrochloride

Ki: 77 nM+

LY310762 HCl

Adrenergic Receptor

Phase 3++++ Ki: 0.04 nM
+

阻害選択性

Phase 3

SETD7/9

Ki: 40.2 nM

Adrenergic Receptor
Inhibitor Name

D2 receptor+++ Ki: 0.61 nM

Ramosetron Hydrochloride

Atomoxetine HCl

5-HT5

Sodium channel

Loxapine Succinate

Desvenlafaxine Succinate

5-HT7

IC50: 240 μM

Azasetron HCl

Citalopram HBr

5-HT6

Fluvoxamine maleate√

Phase 4

Maprotiline HCl

Clomipramine HCl√

Phase 4

Sotalol HCl

Phase 4D3 receptor,D2 receptor

Phase 3Phase 4++++ Ki: 0.7nM
Phase 3++++ Ki: 0.76 nM

Phase 4Phase 4√Phase 4√Phase 4√Phase 4√Phase 3√√

Potassium channel

Phase 4Phase 4Tropisetron HCl√

Phase 4

Phenoxybenzamine HCl

Ondansetron HCl√

Phase 4

Acebutolol HCl√

Phase 4Phase 4

Metroprolol succinate√

Phase 4Phase 4Landiolol hydrochloride√

Duloxetine HCl√

Ondansetron√

Nafronyl oxalate salt
Duloxetine√

Metoprolol√

Dapiprazole Hydrochloride

norepinephrine reuptake√√

Granisetron√

Phase 4

Atipamezole√

Alosetron Hydrochloride√

Phase 2

Atipamezole hydrochloride√

Phase 4

Labetalol HCl√

Phase 4Carteolol HCl

Phase 4

Tolazoline HCl

Cyclobenzaprine HCl√

Palonosetron HCl
Trazodone HCl√√

Cisatracurium Besylate

阻害選択性

Ivabradine HCl

Inhibitor NameNMDA receptor

AMPA receptor

mGluR5(-)-Huperzine A (HupA)
CTEP (RO4956371)

60

GluR
+++

Other Targets

Clinical Phase

Phase 4√Phase 4Phase 4√

Betaxolol

Yohimbine HCl

Phase 4√√Esmolol HCl

GluR

Phase 4√√Phase 3Phase 4√√Phase 4

Ki: 7 nM++++ IC50: 2.2 nM

61

AChR

Dopamine Receptor

阻害選択性

阻害選択性

Inhibitor Name

AChR

mAChR

nAChR

AChE

Donepezil HCl+++(-)-Huperzine A (HupA)++++ Ki: 7 nM++

PNU-120596

Other Targets

IC50: 8.12 nM

Clinical Phase
Phase 4++++++ IC50: 2.5 nM

Phase 4

Aclidinium Bromide++++ Ki: 0.16 nM

Phase 4

Scopolamine HBr+++

Phase 4+

IC50: 5.5 μM

Phase 4++++ Kb: 0.84 nM

5-hydroxymethyl Tolterodine
Gallamine Triethiodide

IC50: 55.3 nM+++++ pKi: 8.9

Phase 4++Jatrorrhizine chloride

IC50: 872 nM
5-HT3 receptor++++ Ki: 6.9 nM

Tropisetron++++ IC50: 6.7 nM

Donepezil
Acotiamide++

IC50: 3 μM

Jatrorrhizine++

IC50: 872 nM++

Palmatine+

Loganin++

Itopride hydrochloride+

Vinblastine sulfate+++

Benzethonium Chloride+

Flavoxate HCl+++

IC50: 162.5 nM

Homatropine Methylbromide+++

IC50: 162.5 nM

BChE,BACE1
dopamine D2-receptor

IC50: 8.9 μM

Phase 3Phase 4

IC50: 49 nM

5-HT3,Sodium channel,
NMDA receptor

IC50: 45.5 μM

Phase 4

IC50: 8 nM

Phase 4

Tiotropium Bromide hydrate√

Phase 4

Fesoterodine Fumarate√

Phase 4Tolterodine tartrate√

Phase 4

Pancuronium dibromide√

Paroxetine HCl

√

5-HT

Phase 4

Amfebutamone (Bupropion) HCl√

Dopamine receptor

Phase 4

Oxybutynin√√

Solifenacin succinate
Trospium chloride

Phase 4Phase 4

Ipratropium Bromide√

Methscopolamine√

Rocuronium Bromide

Phase 4√Phase 4√√

Pyridostigmine Bromide√

Phase 4

Neostigmine Bromide√

Phase 4Phase 1+++ Ki: 18 nM√

Phase 3√Dehydroevodiamine hydrochloride++++ Ki: 2.96 nM+++ Ki: 24 nM

lurasidone++++ Ki: 1 nM

Perospirone hydrochloride++++ Ki: 1.4 nM++

Tetrahydroberberine+++

Ropinirole HCl+++ Ki: 7.5 nM

5-HT6,H1 receptor,5-HT7

Phase 3

5-HT7,5-HT2A,5-HT1A

Phase 4

5-HT2 (human),
5-HT2 (bovine)
5-HT7 receptor,5-HT2A,
5-HT1A receptor
5-HT2 receptor,
5HT1A receptor

Phase 4Phase 4

5-HT1A

Rotundine++ IC50: 166 nM +Olanzapine√

Ki: 29 nM

Phase 4

IC50: 1.47 μM +IC50: 3.25 μM

5-HT1A
5-HT2

Phase 4

Quetiapine Fumarate√

Adrenergic Receptor,
Histamine receptor

Phase 4Chlorpromazine HCl√

Potassium channel

Phase 4

Amfebutamone (Bupropion) HCl

√

AChR

Phase 4

Ziprasidone HCl√

5-HT receptor

Phase 4√Phase 4

Paliperidone
Amisulpride√

Phase 4√Phase 4

Phenothiazine√

Levosulpiride√

Molindone hydrochloride√

Sulpiride√

Phase 4

Prochlorperazine dimaleate salt√

Phase 4

Metoclopramide HCl√

Phase 3Phase 4

Alizapride HCl√

Azaperone√

Phase 4

Opioid Receptor
阻害選択性
Inhibitor Nameδ-opioid receptor

κ-opioid receptor

μ-opioid receptor

JTC-801
Naltrexone HCl
Alvimopan dihydrate (LY246736 dihydrate)

ORL1
+

+++
+++

Ki: 4.4 nM++

Opioid receptor

Clinical Phase

IC50: 94 nM

IC50: 8 nM+++

IC50: 8 nM

Phase 4++++ Ki: 0.77 nM

Ki: 40 nM

Naloxone HCl√

Phase 4

Racecadotril√

Phase 4GABA Receptor
阻害選択性
GABA receptor(+)-Bicuculline++√√

Phase 4

Flumazenil

Pentoxyverine Citrate√

Phase 1

Niflumic acid√

Securinine√

Dopamine subtype 2
receptor√√√

Other Targets

Clinical Phase

Autophagy,HDAC

Phase 4

Ki: 14.5 μM

Phase 4√

Thiocolchicoside√

CatharanthineGABAA receptor+++ IC50: 2 μM

Ginkgolide A

Diphenidol HCl

62

Clinical Phase+ Ki: 1.6 μM

Valproic acid sodium salt (Sodium valproate)√+++ Ki: 9 nM

pKi: 6.08

Phase 3

Orphenadrine Citrate+++ Ki: 4.56 nM

Ki: 1.6 μM√

Oxybutynin hydrochloride

Other Targets

Phase 4+++ Ki: 24 nM

Umeclidinium bromide

Diphemanil Methylsulfate

D4 receptor++++ IC50: 1.68 nM

Inhibitor Name√

Huperzine B

Hexamethonium Dibromide

Dopamine
receptor

Phase 4PDE

Irsogladine

Revefenacin

Loxapine Succinate

DAT

Phase 4√

Otilonium Bromide

D5 receptor++++ IC50: 1.1 nM

Domperidone

IC50: 7.5 nM+++

Tropicamide

IC50: 2.04 μM

BChE

Phase 4+

Procaine HCl+++

IC50: 3.95 μM

Phase 4

IC50: 12.2 μM

Homatropine Bromide

Hyoscyamine

IC50: 0.51 μM

Phase 4D3 receptor++ IC50: 118 nM

Lurasidone HCl

Penfluridol

IC50: 68.0 μM

Darifenacin HBr

D2 receptor

Benztropine mesylate

Chlorprothixene

IC50: 0.35 μM

Atropine sulfate monohydrate

Rivastigmine Tartrate

D1 receptor

Trifluoperazine 2HCl

EC50: 216 nM

Galanthamine HBr

Inhibitor Name

COX-2

√

Homotaurine√

Phase 4

Pentylenetetrazol√

Phase 4Bemegride

Phase 4Phase 3Phase 2

√

63

P-gp

NMDAR

阻害選択性

阻害選択性
Clinical Phase

Inhibitor Name

Zosuquidar (LY335979) 3HCl

Inhibitor Name++

P-gp
Ki: 60 nM

Phase 3(-)-MK 801 maleate++++ Ki: 30.5 nM

Tariquidar+++

Kd: 5.1 nM

Phase 3(+)-MK 801 maleate+++

Kd: 37.2 nM

Elacridar (GF120918)√

Ifenprodil Tartrate+++

IC50: 0.3 μM

SC144

√

Procaine HCl++

IC50: 0.296 mM

Schisandrin B (Sch B)√

Felbamate+

IC50: 1.8 mM

Tiletamine Hydrochloride√

6-Methoxy-2-naphthoic acid√P2 Receptor

Mephenesin√

Linalool√

阻害選択性

Spermidine trihydrochloride√

Autophagy

Kynurenic acid√glutamate receptors,α7 nicotinic acetylcholine receptor

Inhibitor Name

Other Targets

BCRP

ATR

P2 receptor

P2X receptor

P2Y receptor

MRS 2578++

Ticagrelor
Ticlopidine HCl

Clinical Phase

Phase 4+++ IC50: 9 nM

A-317491+++ Ki: 9 nM

A-438079 HCl++

Clinical Phase

Phase 2
5-HT3,nAChR,Sodium channel

Phase 4Phase 2Phase 1

Phase 4

IC50: ~2 μM

A-804598

Other Targets

IC50: 37 nM++++ Ki: 2 nM+

NMDA receptor

CaMK
阻害選択性
Inhibitor Name

pIC50: 6.9

CaMKII

CaMKIII

Prasugrel√

Phase 4

NH125

Clopidogrel√

Phase 4

STO-609

Cangrelor Tetrasodium√

Phase 4

KN-62+

Ki: 0.9 μM

Prasugrel Hydrochloride√

KN-93 Phosphate++

Ki: 0.37 μM

OX Receptor+++

CaMKKαCaMKKβOther Targets

IC50: 60 nM+++

Ki: 0.25 μM++++ Ki: 47 nM
CaMKⅠ,P2RX7,CaMKⅣ

GlyT

阻害選択性

阻害選択性

Inhibitor Name

OX1 receptor

OX2 receptor

Clinical Phase

Almorexant HCl+++

IC50: 6.6 nM++++ IC50: 3.4 nM

Phase 3

SB408124++

Ki: 27 nM

SB-334867√

Inhibitor Name

GlyT1

Amoxapine++

Bitopertin++++ IC50: 22 nM

IC50: 1 mM

Sarcosine

√

BACE

注釈：

阻害選択性

3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

GlyT2

Other Targets

Clinical Phase+++ IC50: 92 μM
Phase 3N-methyl-D-aspartate receptor,GlyR

Phase 2

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。

Inhibitor NameBACE

Other Targets

Clinical Phase

LY2886721+++

IC50: 10.2 nM

LY2811376++

IC50: 239 nM-249 nM

Loganin+

IC50: 47.97 μM

Verubecestat (MK-8931)++++ Ki: 0.37 nM

Phase 3Lanabecestat（AZD3293, LY3314814）+++

Ki: 0.4 nM

Phase 1

Verubecestat (MK-8931) Trifluoroacetat++++ Ki: 0.37 nM

Phase 3

AZD3839++

Ki: 26.1 nM

Phase 1

Phase 2AβPhase 1Substance P
阻害選択性
Inhibitor Name

Substance P

Aprepitant+++

Netupitant√

64

IC50: 0.1 nM

Other Targets
Phase 4Phase 365

NF-κB

阻害選択性
Inhibitor Name
Bay 11-7085

TNF-alpha Inhibitors
Lenalidomide
Pomalidomide
Thalidomide

TNF

Growth Factors

Ag-MHC

PLC γ2RIP
RIPK1

PLC γ2NIK

PKCβ PKCζ

Akt
IKKβ
IKKγ
NEMO

PKR

P65/RelA
NF-κB2
P50/52ATM

HDAC

Immune Regulation Survival

p38 MAPK

P65/RelA
NF-κB2 NF-κB2
P50
P52

NF-κB2
P52

Proliferation

IKKα

MSK1

IKKα/βPan-HDAC Inhibitors
Vorinostat
Entinostat
Panobinostat
Selective HDAC Inhibitors
RGFP966 (HDAC3)
Nexturastat A (HDAC6)
PCI-34051 (HDAC8)Inflammation

UV
GSK-3βIκBαPan-IκB/IKK Inhibitors
IKK-16
Bardoxolone Methyl
Selective IκB/IKK Inhibitors
TPCA-1 (IKK-2)
IMD 0354 (IKK-2)

PI3K

PKC8

MEKK3

IKKα

LT, CD40L,
BAFF/BLysPKC Inhibitors
Enzastaurin
Sotrastaurin
Go 6983
Staurosporine
Quercetin

TRADD
PI3K

Ag

NF-κB2p100

P65/RelA

NF-κB2
p100
RelB

NF-κB2
p100

RelB

IκB
++

IKK

Other Targets

Clinical Phase

IC50: 10 μM

Rosmarinic acid+

MRT67307 HCl+++ IC50: 160 nM

PS-1145+++ IC50: 88 nM

LY2409881++++ IC50: 30 nM

IMD 0354√

Bardoxolone Methyl√

Mesalamine√

Phase 4

Dehydrocostus Lactone√

Phase 2

AZD3264

√

WS6

√

EBP1

WS3

√

EBP1

IC50: 12 μM

Phase 4

NF-κB,Nrf2

Phase 3

NOD1
阻害選択性

RelB
NF-κB Inhibitors
QNZ
Sodium 4-Aminosalicylate
JSH-23SC75741

Lymphogenesis B Cell Maturation

Inhibitor Name
ML130 (Nodinitib-1)

NOD1
+++

IC50: 0.56 μM

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

HDAC

詳細情報はP7に記載されています

NF-κB
阻害選択性
Inhibitor Name

NF-κB

Other Targets

Clinical Phase

QNZ (EVP4593)++++ IC50: 11 nM

JSH-23+

IC50: 7.1 μM

CBL0137 (CBL-0137)++

EC50: 0.47 μM

SC75741+++

EC50: 200 nM

Curcumin√Sodium 4-Aminosalicylate√

Caffeic Acid Phenethyl Ester√

Phase 4

Sodium salicylate√

Phase 1

Pyrrolidinedithiocarbamate ammonium√(-)-Parthenolide√

Andrographolide

√

TNF-α

FACT,p53

Phase 1

HDAC,Nrf2,p300 histone acetylatransferase

Phase 4Phase 3
p53,MDM2 ubiquitination,HDAC1
Phase 4IκB/IKK
阻害選択性
Inhibitor NameBAY 11-7082

IκB
++

IKK

IC50: 10 μM

IKK-16 (IKK Inhibitor VII)+++ IC50: 40 nM

TPCA-1++++ IC50: 17.9 nM

BMS-345541++

IC50: 0.3 μM

SC-514++

IC50: 3 μM-12 μM

66

Other Targets

Clinical Phase

E2-conjugating enzymes

CDK2/CyclinA,AUR2,PRAK

67

Metabolism

P450 (e.g. CYP17)
阻害選択性
M2 Macrophage
IL-10(to Other(Anti-inflammatory)
Organs)TNF-alpha Inhibitors
Lenalidomide
Pomalidomide
Thalidomide

CD36

Insulin

TNFα

GlucoseInsulin R

β3AR

TNFR

BCAAs

S1P

Adiponectin
Adipo R

AC Gsα
cAMP

PKA
CIDEA

HSL

ATGL

Insulin
Signaling

Pan-Akt Inhibitors
MK-2206
Perifosine
GSK690693
Selective Akt Inhibitors
A-674563 (Akt1)
CCT128930 (Akt2)

CGI-58GlucoseHIF-1αDestabilization

AcetylCoA

CDK5

PPARγ

Autophagy

PGC-1α + PPARγ

NAD+/NADH

Mitochondrial
Biogenesis
Program

IKK

NEMO

ROS

Mitochondria(Normal Function)

UCP1

NF-κB-mediatedInflammation
Adipocyte-specific
Gene Expression

C/EBPβC/EBPαChaperones Regulating
Adiponectin Secretion

PPAR Agonists
Rosiglitazone
GW0742 (PPARβ/δ)PPAR Antagonists
GW9662
FH535

Phase 4+

Avasimibe

IC50: 13.9 μM

+

ACAT

IC50: 2.9 μM

Ketoconazole+

Casein Kinase

IC50: 0.19 mM

Testosterone 6 beta-hydroxylase

TAK-700 (Orteronel)

Phase 3+++ 20-lyase (Rat)++++

Phase 4Phase 4++++ IC50: 6.1 nM

Androgen Receptor

IC50: 300 nM

Phase 3Phase 4

IC50: 30 nM-285 nM

Ozagrel++++ IC50: 11 nM

Phase 4

Ozagrel HCl++++ IC50: 11 nM

Phase 4

Alizarin++

7-Hydroxyflavone+++ Ki: 0.015 μM

IC50: 2.7 μM

Diallyl sulfide+

IC50: 17.3 μM

Sulfaphenazole++

Ki: 0.3 μM

Benzbromarone+++ Ki: 19.3 nM

Phase 4+++ IC50: 30 nM++

Ki: 2 μM

Ritonavir√

Posaconazole√

HIV

Phase 4

lanosterol 14α-demethylase

Phase 4

Voriconazole√

Phase 4

Fluconazole√

Phase 4Phase 4√

Thiabendazole√

Methoxsalen

CYP2A5√

Acetylshikonin

Phase 4√

Gentiopicroside√

Sodium Danshensu√

Naringenin√

Diosmetin√

Phase 1

Piperine

Phase 2√√

Baicalein

詳細情報はP40に記載されています

Clinical Phase
Phase 4

Naringin

HSP (e.g. HSP90)

Other Targets+++ IC50: 72 nM

Clarithromycin

Pan-mTOR Inhibitors
AZD8055
KU-0063794
PP242
Selective mTOR Inhibitors
Rapamycin (mTORC1)
Everolimus (mTORC1)

ROS

PPARγ

NF-κB

P450

Abiraterone Acetate

ApigeninpSTAT3BCAA
Catabolism

FA
Oxidation

CYP17++++ IC50: 2 nM

Cobicistat (GS-9350)

GOLGI

CPT1

pCREB
SIRT1

TLR4

IRAK TRAF6mTORC

AcetylCoA

PDH

CYP3

PF-4981517

MalonylCoA

CitrateNormalOxidative
Stress[AMP:ATP]TCS1/2OXPHOS

IL-6

JAK-STAT
MYD88
Glut4
Translocation
Ceramide

LKB1

CYP2

Itraconazole

Ca2+

CAMKKβ

AMPK

SIRT1

Pyruvate

Cytosol
Nucleus

PKCθ/
PP2A

ACC

O2
(Normoxia)
Perilipins

IRS1
PI3K

pAkt

PKA Inhibitors
A-674563
H 89
AT13148MGL
LIPID
DROPLET

SOCS3

S1P

Ceramide

p38 MAPK

GlucoseGlycerol
Neogenesis

FSP27

TG

ATP

Lipogenesis

FAs

JNK

CYP1

Abiraterone

Galeterone

SLC6

FATP

Caveolins
Lipolysis

Adiponectin
Release Saturated
FAs

FGFRs/
βKlotho

S1PR

Glut4

LPL

FGF21

gp130
IL-6R
gp130

Lipoprotein SNS Signaling
Particles

FAs

Inhibitor Name√

PDE

詳細情報はP56に記載されています

阻害選択性
Inhibitor Name

PPAR
PPARα
+++

PPARβ/δPPARγ+++

IC50: 32 nM

PPARδ

Other Targets

Clinical Phase

IC50: 3.3 nM++++ IC50: 1 nM

T0070907
GSK3787++

Harmine

FH535

PDE2

PDE3

PDE4

pIC50: 6.6

pIC50: 6.6
MAO-A

√

Wnt/β-catenin

Phase 4√

Other
Targets

Clinical Phase

Phase 4+++ IC50: 33 nM

Phase 3

Tadalafil++++ IC50: 1.8 nM

Phase 4

Vardenafil HCl
Trihydrate++++ IC50: 0.7 nM

Phase 4++ IC50: 0.32 μM
Phase 2++++ IC50: 3.2 pM

Mardepodect(PF-2545920)++++ IC50: 0.37 nM

Rolipram++

Cilostazol

IC50: 130 nM++ IC50: 5.2 μM

ATPaseFenspiride HCl+++

IC50: 0.75 μM
adenosine
receptor

IC50: 0.12 mM+ pIC50: 3.44+

Phase 4Phase 4++++ IC50: 1 nM

S- (+)-Rolipram

Phase 2Phase 4++ IC50: 2.1 μM

AvanafilAminophylline

PDE4D++ IC50: 0.2 μM

Milrinone68

PDE10A+++ IC50: 100 nM

GSK256066√

PDE6

Phase 4+++ IC50: 3.5 nM

Cilomilast

Pimobendan

++

PDE5

++++ IC50: 0.7 nM

Sildenafil Citrate

Inhibitor Name

Fenofibric acid

PDE1

Roflumilast

阻害選択性

GW9662

PDE

Phase 4

pIC50: 4.16

69

Dehydrogenase

阻害選択性
Inhibitor Name

PDE

Ibudilast

PDE1

PDE2

PDE3

PDE4

+++ IC50: 0.11 μM

PDE5+++ IC50: 0.08 μM ++

PDE6

Other
Targets

PDE10A

Clinical Phase

IC50: 2.2 μM

阻害選択性
Inhibitor Name

Dehydrogenase

Mycophenolate Mofetil+++

IC50: 27 nM

AGI-5198++

IC50: 70 nM

MK-8245++++ IC50: 1 nM

NCT-503+

IC50: 2.5 μM

ML390

+

IC50: 0.56 μM

Enasidenib (AG-221)++++ IC50: 12 nM

NCT-501++

SW033291++++ IC50: 1.5 nM

Vidofludimus++

IC50: 134 nM

AGI-6780+++

IC50: 23 nM

Daidzin+++Ki: 20 nM

CPI-613√

Phase 3

Leflunomide√

Phase 4

Mycophenolic acid√

Phase 4

Hydroxylase

Disulfiram√Phase 4

Trilostane√

Phase 2

阻害選択性

Teriflunomide√

Phase 4

PluriSIn #1 (NSC 14613)√

Ammonium Glycyrrhizinate√

Gimeracil√

3-Nitropropionic acid√

Vorasidenib (AG-881)√

RRx-001√

Ivosidenib (AG-120)√

Isovaleramide√

gossypol-Acetic acid√

Enoxolone√

Emodin√Fomepizole√

TAK-063++++ IC50: 0.3 nM

Sildenafil

Phase 2+++ IC50: 5.22 nM

PF-8380++++ IC50: 2.8 nM

Deltarasin+++ Kd: 38 nM

Luteolin+ Ki: 15.0 μM +Ki: 6.4 μM+ Ki: 13.9 μM+

Ki: 11.1 μM

IcariinPhase 4+

Ki: 9.5 μM

Phase 2++

IC50: 0.432 μM

Phase 3

Anagrelide HCl√

Phase 4

Irsogladine√

Doxofylline√

Phase 4

Dipyridamole√

Phase 4Dyphylline√

mAChR,AChR

Crisaborole (AN2728)√

Sildenafil Mesylate√

Inhibitor Name

Hydroxylase

Clinical Phase

Nepicastat (SYN-117) HCl+++

IC50: 8.5 nM

Phase 2

Osilodrostat (LCI699)++++ IC50: 2.5 nM

Phase 3

Ro 61-8048+++

IC50: 37 nM(R)-Nepicastat HCl++

IC50: 18.3 nM

Tetrahydropapaverine HCl+

IC50: 5.7 μM

Mildronate√

4-Chloro-DL-phenylalanine

√

DMOG

√

Telotristat Etiprate (LX 1606 Hippurate)√

Phase 2Phase 3Phase 1Other Targets

Clinical Phase
Phase 4Phase 2Phase 3

IC50: 40 nM

Phase 2Phase 1

Phase 3Phase 1
Nrf2-ARE

Phase 3Phase 3

Bcl2

Phase 3Phase 2Phase 2

Factor Xa
阻害選択性
Inhibitor Name

Factor Xa
IC50: 0.7 nM

Rivaroxaban++

Apixaban++++ Ki: 0.08 nM

Edoxaban+++

Edoxaban tosylate Monohydrate√

Other Targets

Clinical Phase

Prothrombinase

Phase 4Phase 4

Ki: 0.561 nM

Phase 4

Procollagen C Proteinase
阻害選択性
Inhibitor Name

Procollagen C Proteinase

UK 383367+++

Phospholipase (e.g. PLA)

DHFR

阻害選択性

阻害選択性

Inhibitor Name

Inhibitor Name

DHFR

Other Targets
TS,GARFT

Phospholipase (e.g. PLA)

Clinical Phase

Varespladib (LY315920)+++

Phase 4

Darapladib (SB-480848)++++ IC50: 0.25 nM

Pemetrexed++++ Ki: 7.2 nM

Methotrexate++

IC50: 24 nM

Phase 4

Tanshinone I++

Pyrimethamine+++

IC50: 15.4 nM

Phase 4

Halobetasol Propionate√

Methotrexate disodium++

IC50: 24 nM

U73122√Pemetrexed Disodium Hydrate++++ Ki: 7.2 nM

Polydatin√

Pralatrexate√

Diaveridine√

70

IC50: 44 nM

TS,GARFT

Phase 4

IC50: 7 nM

IC50: 11 μM

Clinical Phase
Phase 3Phase 3Phase 4Phase 4Phase 2Phase 471

Carbonic Anhydrase

Lipase

阻害選択性

阻害選択性
Carbonic
Anhydrase

Inhibitor Name

Carbonic
Anhydrase I

Dorzolamide HCl+

Carbonic
Anhydrase II

Carbonic
Anhydrase IV++++ Ki: 1.9 nM

Ki: 6000 nM+

Other Targets Clinical Phase
Phase 4++

Tioxolone

Carbonic
Anhydrase XII+++ Ki: 31 nM

U-104

Ki: 45.1 nM++++ Ki: 4.5 nM

Ki: 91 nM

Brinzolamide
Acetazolamide

Carbonic
Anhydrase IX++++ IC50: 3.19 nM+++ IC50: 10 nM

Methazolamide++

Topiramate√

Dichlorphenamide√

Mafenide Acetate√

Benzenesulfonamide√+++ Ki: 14 nM

Ki: 50 nM++

Ki: 36 nM

Inhibitor Name

LipaseJZL184++++ IC50: 8 nM

Atglistatin++

IC50: 0.7 μM
IC50: 0.237 μM

XEN445+++Phase 4

Orlistat√Phase 4

Tanshinone IIA√

Clinical Phase

Fatty acid synthesis

Phase 4Phase 4Phase 4
sodium channel,
AMPA/kainate receptor,
Calcium Channel

Phase 4Phase 3

Transferase
阻害選択性
Inhibitor Name

MAO
阻害選択性
Inhibitor Name

MAO-A

MAO-B

MAO

Other Targets

Clinical Phase++++ IC50: 98 nM

Safinamide Mesylate
Rasagiline Mesylate+++

IC50: 412 nM++++ IC50: 4.43 nM

Tranylcypromine (2-PCPA) HCl++

IC50: 11.5 μM+++

Moclobemide (Ro 111163)+++

IC50: 6.1 μM

Phase 4

IC50: 7 μM

Phase 4LSD1Phase 3++++ Ki: 16.7 nM

Safinamide
Harmine++++ Ki: 0.048 μM

Pargyline hydrochloride++

Ki: 13 μM+++

Ki: 0.5 μM

Isatin+

IC50: 58 μM++

IC50: 14 μM

IC50: 15 μM+

IC50: 17 μM

Glycyrrhizin (Glycyrrhizic Acid)+++

IC50: 0.16 μM

Iproniazid√

Sennoside A+

Transferase

Clinical Phase

Tipifarnib+++

IC50: 0.6 nM

Phase 3Lonafarnib+++

IC50: 1.9 nM

Phase 3

Daporinad (FK866, APO866)++++ Ki: 0.4 nM

A922500++

IC50: 7 nM

Lomeguatrib++

IC50: 5 nM

FTI 277 HCl++++ IC50: 500 pM

LB42708+++

IC50: 1.2 nM

PF-04620110+

IC50: 19 nM

Phase 1

Tolcapone+

Ki: 30 nM

Phase 4

GGTI 298 TFA salt√

Phase 2PPARγ++

Paeonol

Other Targets

IC50: 54.6 μM+

Ferroptosis
阻害選択性IC50: 42.5 μM
11 beta-hydroxysteroid
dehydrogenase,HMGB1

Phase 4

Liver X Receptor

Inhibitor Name

Ferroptosis

Ferrostatin-1 (Fer-1)++

EC50: 60 nM

Liproxstatin-1+++

IC50: 22 nM

Lipoxygenase

阻害選択性
Inhibitor Name

阻害選択性

Liver X Receptor

SR9243

Inhibitor Name√lipoxygenase
IC50: 29.5 μM

Other Targets

Clinical Phase

Abietic Acid

+++

FAAH

Zileuton√

Phase 4

Nordihydroguaiaretic acid (NDGA)√

Phase 2阻害選択性

Esculetin√

MK-886 (L-663,536)√

Inhibitor NameFAAH

URB597++++ IC50: 4.6 nM

PF-3845++

Ki: 230 nM

JNJ-1661010+++

IC50: 10 nM

Biochanin A+

IC50: 1.8 μM

Other Targets

Clinical Phase

HMG-CoA Reductase
阻害選択性

EGFR

CETP
阻害選択性
Inhibitor Name

CETP
+++

IC50: 7.9 nM

HMG-CoA Reductase

Other Targets

Clinical Phase

Simvastatin++++ Ki: 0.1-0.2 nM

Rosuvastatin Calcium+++

IC50: 11 nM

Phase 4Phase 4Phase 4

Lovastatin++++ IC50: 3.4 nM

Clinical Phase

Fluvastatin Sodium+++

IC50: 8 nM

Phase 4Phase 3

Pravastatin sodium++

IC50: 5.6 μM

Phase 4+

IC50: 0.47 mM
IC50: 850 nM

Torcetrapib++

IC50: 37 nM

Phase 3Clinofibrate

Evacetrapib (LY2484595)++++ IC50: 5.5 nM

Phase 3SR-12813++

Dalcetrapib (JTT-705, RO4607381)+

IC50: 0.2 μM

Phase 3

Pitavastatin Calcium√

72

PPARα,COX-1,COX-2

Phase 1

Inhibitor Name

Anacetrapib (MK-0859)

PPARγ

pregnane X receptor
cholesterol esters

Phase 4

73

PKM

阻害選択性
Inhibitor Name

HMG-CoA Reductase

Atorvastatin Calcium√

Mevastatin√

Rosuvastatin

Other Targets

Clinical Phase
Phase 4√Phase 4

阻害選択性
Inhibitor Name
PKM2 inhibitor(compound 3k)

PKM2
+++

IC50: 2.95 μM

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

AhR

2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

阻害選択性
Inhibitor Name

AhR

StemRegenin 1 (SR1)++

IC50: 127 nM

CH-223191+++

IC50: 30 nM

UM729

√

Clinical Phase
Phase 2

NAMPT
阻害選択性
Inhibitor Name

NAMPT

KPT-9274++

IC50: ~120 nM

GMX1778 (CHS828)+++

IC50: <25 nM

STF-118804√

Other Targets

Clinical Phase

PAK4
Phase 1IDO
阻害選択性
Inhibitor Name

IDO

Clinical Phase

NLG919+++BMS-986205++++ IC50: 1.7 nM

IDO inhibitor 1+++

IC50: 3 nM

PF-06840003+

IC50: 0.41 μM

Phase 1

Epacadostat (INCB024360)++

IC50: 10 nM

Phase 3

INCB024360 analogue++

IC50: 67 nM

Phase 2Indoximod (NLG-8189）√

EC50: 75 nM
Phase 3Phase 3

Decarboxylase
阻害選択性
Inhibitor Namedecarboxylase

Carbidopa+++

Benserazide HCl√

Eflornithine hydrochloride hydrate√

Methyldopa√

Clinical Phase

IC50: 29 μM

Phase 4Phase 4Phase 4GLUT
阻害選択性
Inhibitor Name

GLUT1

BAY-876+++

IC50: 0.002 μM

WZB117++

IC50: 10μM

STF-31√74

75

GPCR & G Protein
Smoothened Antagonists
Cyclopamine
LDE225
LY2940680
BMS-833923
Smoothened Agonist
Purmorphamine

Hedgehog

HB-EGF MMPs

Smo

PTC

Endothelin Receptor
阻害選択性
5-HT Receptor Antagonists
Clozapine
Olanzapine
Ketanserin
5-HT Receptor Agonists
Prucalopride
WAY-100635
Eletriptan

5HT2B

ET1

EGFR

βγ

PI3K
Akt

βγ

Src

αq

βγ

SHC

PI3K

AC

β-arrestin

JAK
Ras

cAMP
PKA

Glutamate

Src

Akt
STAT

cAMP Activator
Forskolin

Raf
MEKs

GEFs

Thrombin

AC

IP3

Ca2+

Raf

mTOR

βγ

αi

ERK

ERK

GEFs

PI3K CDC42
cAMP
PKA

ET-A

Zibotentan (ZD4054)++

IC50: 21 nM

Bosentan Hydrate+++

Ki: 4.7 nM

Macitentan++++ IC50: 0.5 nM

Bosentan+++Ki: 4.7 nM

BQ-123+++

IC50: 7.3 nM

Ambrisentan

√

ET-B

Rac

Rho

PAK

Phase 3
Ki: 95 nM

Phase 4+

IC50: 391 nM

Phase 4++

Ki: 95 nM

Phase 4Phase 2Phase 4

S1P Receptor
阻害選択性
Inhibitor Name
Fingolimod (FTY720) HCl

S1PR

S1PR1

S1PR5

SphK

ROCK

Clinical Phase
Phase 4+++

Ponesimod++

EC50: 5.7 nM

Ozanimod (RPC1063)+++

EC50: 0.41 nM

IC50: 2.0 nM
Phase 3++Phase 3

EC50: 11 nM+++++ EC50: 0.39 nM

BAF312 (Siponimod)

ERK

S1PR2

++++ IC50: 0.033 nM

JTE 013

p38

Rho

Clinical Phase++

PF-543

MEKs

MEKs

NF-κB

α12

Src

GEFs

p70S6K

βγ

PLCβ

PKC

IKKs

αs

DAG

Ras

MEKs

GLI

5HT1D

GPCR

SOS
GRB2

αi

Inhibitor Name

Endothelin Receptor
Antagonists
Zibotentan
Bosentan
Macitentan
Sitaxentan+++

IC50: 17 nM
Phase 3

EC50: 0.98 nM

Opaganib (ABC294640)+

Phase 2

IC50: 60 μM

ROCK

SGLT
Transcription Factors

阻害選択性
Inhibitor Name

Proliferation, Survival, Invasion,
Migration, Angiogenesis

Gene Expression

5-HT Receptor

Adrenergic Receptor

詳細情報はP59に記載されています

詳細情報はP61に記載されています

Dopamine Receptor

Opioid Receptor

Hedgehog/Smoothened

詳細情報はP19に記載されています

Phase 4+++

IC50: 3.7 nM

Phase 4

Empagliflozin (BI 10773)++

IC50: 3.1 nM

Phase 4

Ertugliflozin++++ IC50: 0.877 nM

Ipragliflozin (ASP1941)+

IC50: 7.4 nM

Tofogliflozin(CSG 452)++

IC50: 2.9 nM

Phase 4+++

IC50: 1.8 nM

Phase 3+

IC50: 36 nM

Phase 4mouse SGLT2,rat SGLT2Phase 4√√

LPA Receptor
阻害選択性
Inhibitor Name

CXCR

詳細情報はP64に記載されています

Clinical Phase++++ EC50: 1.1 nM

Phloretin

詳細情報はP56に記載されています

OX Receptor

Other Targets

Canagliflozin

Dapagliflozin propanediol monohydrate

詳細情報はP63に記載されています

詳細情報はP63に記載されています

SGLT2

Dapagliflozin

Sotagliflozin (LX4211)

Histamine Receptor

SGLT1

詳細情報はP20に記載されています

Cannabinoid Receptor

LPA1

Ki16425+++

Ki: 0.34 μM

Ki16198+++

Ki: 0.34 μM

ONO-7300243++++ IC50: 0.16 μM

LPA2+

Ki: 6.5 μM

LPA3
++

Ki: 0.93 μM++

Ki: 0.93 μM

PAFR

阻害選択性

阻害選択性
Inhibitor Name

CB1
IC50: 13.6 nM

Rimonabant+++Otenabant (CP-945598) HCl++++ Ki: 0.7 nM

AM251

√

Olivetol

√

76

CB2
++

Other Targets

IC50: 1.64 μM

Clinical Phase
Phase 4Phase 3

Inhibitor Name
Ginkgolide B

PAFR
+++

IC50: 3.6 μM

CYP1A1,CYP2C19

77

Endocrinology & Hormones

PKA
阻害選択性
Inhibitor Name

PKA

Other Targets

A-674563+++

Ki: 16 nM

Akt1,CDK2,GSK-3β

H 89 2HCl++

Ki: 48 nM

S6K1

Daphnetin+

IC50: 9.33 μM

EGFR,PKC

AT13148++++ IC50: 3 nM

Clinical Phase

Growth Factors
RTKs

Estrogen
GPCR

P

Phase 1

ROCK2,ROCK1,p70S6K

Adenosine Receptor

cAMP

阻害選択性
Adenosine Receptor

Other Targets+++

Ki: 2.2 nM

Phase 3

AZD-4635 (HTL1071)++++ Ki: 1.7 nM

Phase 2A2AR antagonist 1++

Ki: 4 nM

SCH58261+++

Ki: 2.0 nM

Reversine+

Ki: 0.66 μM

Proxyphylline√

ZM241385

√

Akt

PI3K

Pan-PI3K Inhibitors
BEZ235
GDC-0941
LY294002
Selective PI3K Inhibitors
HS-173 (p110α)
TGX-221 (p110β)
CZC24832 (p110γ)
CAL-101 (p110δ)

Pan-Akt Inhibitors
MK-2206
Perifosine
GSK690693
Selective Akt Inhibitors
A-674563 (Akt1)
CCT128930 (Akt2)

Clinical Phase

Istradefylline

eNOS

PKA
P

Aurora A,Aurora B,Aurora C

CREB

Bcl-2

Antiapoptosis

NO

Ras

GRB2

Raf
MEKKs

NPS-2143

+++

JNKs

IKKs

p38

ERK1/2

Estrogen Receptor Antagonists
Fulvestrant
Raloxifene
Tamoxifen
Estrogen Receptor Agonists
Hexestrol
Erteberel
Estradiol Valerate

HSP

MEK

p300

T

ERK1/2

AR

AR

E6AP

BRCA1
RP-A

ER
PGC1

RTA

SRC1 TIF2
AIB1

Estrogen Estrogen
ER

Androgen Receptor
Antagonists
Enzalutamide
Bicalutamide
Galeterone
AZD3514
Androgen Receptor Agonist
Andarine

Cyclin D1

NCOR

Sim3
HDACs

cAMP
PKA

DHT

PELP1

Akt

Src

ctase

HSP

BRG1

PI3K

STAT3

P

edu

5α-R

5-alpha Reductase
Inhibitors
DutasterideFinasteride

NF-κB

Vasodilation

ER

SHP

SRA

P6S
TRAP220

AR
AR

p72
REA
DAX1 RIP140

Opioid Receptor

阻害選択性
Inhibitor Name

Estrogen

EstrogenIC50: 43 nM

Vasopressin Receptor

JAK1

ER

Gene
Expression

CaSR

Ras

Pan-Raf Inhibitors
Vemurafenib
Sorafenib
Dabrafenib
Selective Raf Inhibitors
GDC-0879 (B-Raf)
GW5074 (C-Raf)

CREB NF-κB Sp1 c-Jun c-Fos Elk1

阻害選択性

SHC
Src

SOS

MAPKs

CaSR
Inhibitor Name

IGF-1
EGF
RTK

IL-6R

Gα Gβ Gγ

Inhibitor Name

Estrogen

Vasopressin receptor 1

Vasopressin receptor 2

Clinical Phase++++ IC50: 3 nM

Phase 4

Tolvaptan
Mozavaptan++

Conivaptan HCl√

IC50: 1.2 μM+++

詳細情報はP63に記載されています

5-alpha Reductase

IC50: 14 nM
Phase 4

阻害選択性
Inhibitor Name

cAMP
阻害選択性
Inhibitor Name

AC

EPAC1

EPAC2

PACAP 6-38
Bithionol+

Other Targets++++ IC50: 2 nM

CARTp

IC50: 4.0 μM

ESI-09++

IC50: 3.2 μM

HJC0350
PACAP 1-27
SQ22536

PACAP receptor+++

IC50: 1.4 μM+++

IC50: 0.3 μM

Finasteride+++

Dutasteride√注釈：
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Inhibitor Name

Estrogen receptor

Fulvestrant+++

IC50: 0.94 nM

Raloxifene HCl++

IC50: 5.7 nM

Phase 4Phase 4

Bazedoxifene HCl+

Tamoxifen Citrate√

Toremifene Citrate√

Clomifene citrate

Progesterone receptor

Other Targets

Clinical Phase
Phase 4Phase 4++++ IC50: 0.2 nM

Dienogest

78

Ki: 10.2 nM

Estrogen/progestogen Receptor

Mifepristone

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

Clinical Phase

阻害選択性

√
√

5-alpha Reductase

IC50: 23 nM

Glucocorticoid receptor

Phase 4Phase 4Phase 4Phase 4√√Phase 4Phase 4

Drospirenone√

Phase 4

Ulipristal√

Phase 479

阻害選択性

阻害選択性

Inhibitor Name

Estrogen receptor

Inhibitor Name

Progesterone receptor

Other Targets

Clinical Phase√

Androgen Receptor

Phase 4Azilsartan

Megestrol Acetate√

AT1 receptor+++

AT2 receptor

ACE

Renin

RAAS

Clinical Phase
Phase 4

IC50: 2.6 nM

Phase 4Phase 4

Telmisartan√

Estriol√

Phase 4

Valsartan√

Estrone√Phase 2

Benazepril HCl√

Phase 4

Bazedoxifene Acetate√

Phase 4

Enalapril Maleate√

Phase 4

Cyclofenil√

Olmesartan Medoxomil

PHTPP

√

Cilazapril Monohydrate√

AZD9496√

Phase 1

Lisinopril√

Phase 4Chlorotrianisene√

Phase 4

Moexipril HCl√

Phase 2Endoxifen HCl√

Phase 2

Temocapril HCl√

Ospemifene√

Phase 4

Quinapril HCl√

Tamoxifen√

Phase 4

Delapril Hydrochloride√

Zofenopril calcium√

Pregnenolone

Fimasartan

Androgen Receptor

Phase 4√Phase 4√

Androgen Receptor

Other Targets

IC50: 36 nM

Phase 4

Bicalutamide++

IC50: 0.16 μM

Phase 4

Aromatase

Ostarine (GTx-024, MK-2866 )++++ Ki: 3.8 nM

Phase 3

阻害選択性

Apalutamide (ARN-509)+++

IC50: 16 nM

Galeterone+

IC50: 384 nM

Flutamide+++

Ki: 55 nM

Phase 4

Cyproterone Acetate++++ IC50: 7.1 nM

Phase 4

AZD3514+

Ki: 2.2 μM

Phase 1

Spironolactone++

IC50: 77 nM

Phase 4

Triptophenolide++

IC50: 260 nM

RAD140++++ Ki: 7 nM

EPI-001+

IC50: ~6 μM

Darolutamide (ODM-201)+++

Ki: 11 nM

Dehydroepiandrosterone (DHEA)√

Megestrol Acetate√

RU58841√

Nilutamide√

Phase 2

Inhibitor Name

Phase 3

CYP17

AR-T877A,AR-F876L
Phase 1

Aromatase

Other Targets

Clinical Phase

Letrozole++++ IC50: 0.07 nM-20 nM

Phase 4

Anastrozole+++

IC50: 15 nM

Phase 4

Exemestane+++

IC50: 30 nM

Phase 4Formestane++

IC50: 80 nM

Aminoglutethimide++

IC50: 10 μM

alpha-Naphthoflavone++++ Ki: 5 nM

Obacunone+

Phase 3

IC50: 28.4 μM

Nrf2

PPARγ
Phase 3Phase 4GPR

Phase 4progestogen Receptor

阻害選択性
Inhibitor Name

RAAS
阻害選択性

GPR

Clinical Phase

AZD1981+++

IC50: 4 nM

Phase 2OC000459++

IC50: 13 nM

Phase 2

注釈：

Inhibitor Name

AT1 receptor

AT2 receptor

ACE

Renin
+++

Aliskiren Hemifumarate
Candesartan++++ IC50: 0.26 nM

Losartan Potassium (DuP 753)+

Phase 4

IC50: 1.5 nM

Phase 4

IC50: 34 nM
Phase 3++++ IC50: 1.05 nM++++ IC50: 0.26 nM

Candesartan Cilexetil

Phase 4

Ramipril++

IC50: 5 nM

Phase 4

Captopril++

IC50: 6 nM

Phase 4+++

IC50: 2.6 nM+++

Phase 4

IC50: 2.6 nM

Imidapril HCl

2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Phase 4+

Perindopril Erbumine

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

Phase 4
IC50: 1.94 nM

IC50: 1.3 nM

PD123319

Clinical Phase

Phase 4

+++
+++

RAAS

IC50: 20 nM

Enalaprilat Dihydrate

Phase 3

Losartan+

IC50: 20 nM

Phase 4

Eprosartan Mesylate++++ Kd: 0.83 nM

Phase 480

Phase 4√

Clinical Phase+++

Azilsartan Medoxomil

Phase 4√

Fosinopril Sodium

Enzalutamide (MDV3100)

Irbesartan

Phase 4

Sacubitril/valsartan (LCZ696)

阻害選択性
Inhibitor Name

Phase 481

Transmembrane Transporters
Proton Pump Inhibitors
Lansoprazole
Omeprazole
Esomeprazole Magnesium
Zinc Pyrithione
PF-3716556

MembraneAR

MR/Classical
AR
HSP

Ca2+

PIP5K
KRas2A PI3K

PLC

IPYK

PIP2

IP3

Na+

Raf

PIP3

PKC
MEK

SAH
Hydrolase

HSP

MAPK

Aldosterone
MR/ClassicalAR

Transcription
Factors

Ca2+

NEDD4

Ca2+ Channel

ReceptorGDPγ β αq

Ca
γβ
PLC

PIP2
IP3

SOS

DAG

Calcium Channel Inhibitors
Amlodipine Besylate
Cilnidipine
Isradipine
Felodipine
Calcium Channel Activator
Strontium Ranelate

PKA-C
PKA-R

2+

Contraction

RyR

CaTranslation

Calci-neurin

HDAC4/5

NFAT-3
MCIP-1

Ca

Mitochondria

Transcription
Factors

CaM

Ca2+

Ca
Ca2+
Ca2+
Ca2+ 2+
Ca

Phospholamban
ATP

2+

IP3R

PKC

MKP1

MR/Classical MR/Classical
AR
AR
mRNA
SRE

Ca2+

SERCA

PDK

SGK
Aldosterone

Sodium Channel Inhibitors
Carbamazepine
Phenytoin
A-803467
Procainamide
DigoxinNa+
Na+ Channel

Na+/H+
Transporter

Aldosterone

阻害選択性

CaMKIV

2+

2+

TnC
CaM

PDE

MAPK
Pathway

CaMKII

Ca2+

Inhibitor Name

Calcium Channel

Other Targets

Clinical Phase

Dronedarone HCl√

Potassium channel,Sodium channel

Phase 4

Lacidipine√

Phase 4

Nicardipine HCl√

Phase 4

Clevidipine Butyrate√

Phase 4

Nifedipine√

Phase 4HC-030031√

Benidipine HCl√

Phase 4

Azelnidipine√

Phase 4

Tetracaine HCl√

Phase 4

Fendiline hydrochloride√

Efonidipine

√

ML204

√

Levamlodipine√

Cinnarizine√

Lercanidipine hydrochloride√

SKF96365√

Lomerizine 2HCl√

Cinepazide maleate√

Tetrandrine√

Diltiazem HCl

√

P-gp

詳細情報はP64に記載されています

Calcium Channel
阻害選択性
Inhibitor Name

Calcium Channel

Other Targets

Clinical Phase

Amlodipine Besylate+++

IC50: 1.9 nM

Phase 4

Manidipine 2HCl+++

IC50: 2.6 nM

Phase 4

Felodipine
Manidipine+++++

Nilvadipine++++ IC50: 0.03 nM

Nitrendipine++

Phase 4

IC50: 2.6 nM

Nisoldipine

Flunarizine 2HCl

Phase 4++++ IC50: 0.15 nM

Phase 4

IC50: 10 nM

Phase 3Phase 4

Ki: 68 nM

Phase 4

IC50: 95 nM

Levetiracetam√

Phase 4

Cilnidipine√

Phase 4

Amiloride HCl√

Verapamil HCl√

Sodium channel,uPA

Phase 4Phase 4Ranolazine 2HCl√

Phase 4

Amlodipine√

Phase 4

Isradipine
Ranolazine√√

Phase 3Phase 4

Econazole nitrate√

Phase 3

Nimodipine√

Phase 482

Phase 4Phase 2Phase 4

阻害選択性
Inhibitor Name

詳細情報はP63に記載されています

Histamine receptor

Sodium Channel

CREB

Transcription
Hypertrophy

GABA Receptor

Phase 4

Sodium Channel

Other Targets

Clinical Phase
Phase 4

Carbamazepine++

A-803467++++ IC50: 8 nM

Camostat Mesilate+++

Ouabain++++ Ki: 15 nM

Ambroxol HCl+++

IC50: 35.2 μM-22.5 μM

Triamterene+++

IC50: 4.5 μM

ENaCαS583

Phase 4

Procaine HCl++

IC50: 60 μM

5-HT3,nAChR,NMDA receptor

Phase 4

Proparacaine HCl+

ED50: 3.4 mM

Oxcarbazepine+

IC50: 160 μM

Riluzole√

Bupivacaine HCl√

Amiloride HCl√

Rufinamide√

Phase 3

Zonisamide√

Phase 4

Phenytoin Sodium√

Phase 4

Amiloride HCl dihydrate√

Dronedarone HCl√

Phenytoin√

Lamotrigine√

Primidone√(-)-Sparteine Sulfate√

Quinidine sulfate√

Procainamide HCl√

Mexiletine HCl√

Phase 4

Benzocaine√

Phase 4

Tolperisone HCl√

Phase 2

Levobupivacaine HCl√

Phase 4

Dibucaine HCl√

Ibutilide Fumarate√

IC50: 131 μM

IC50: 50 nM

Phase 3Phase 3Phase 4NMDA receptor,Glutamate release

Phase 4Phase 4

T-type calcium channel,uPA

Phase 4Phase 4
Potassium channel,Calcium channel

Phase 4Phase 45-HT (human platelets),
5-HT (rat brain synaptosomes)

Phase 4Phase 2Phase 3DNA methyltransferase

Phase 4Phase 483

阻害選択性Inhibitor Name

阻害選択性
Sodium Channel

Other Targets

Clinical Phase

Inhibitor Name

Proton Pump

Vinpocetine√

Phase 3

Revaprazan Hydrochloride√

Propafenone HCl√

Phase 4

Rabeprazole√

Ilaprazole√

Rebeprazole sodium√

Pantoprazole sodium√

Tenatoprazole√

ATPase阻害選択性
Inhibitor Name

ATPase+++IC50: 0.2 μM(-)-Blebbistatin+

IC50: 0.5 μM-5 μM

Sodium orthovanadate+++

IC50: 40 nM

PF-3716556++

pIC50: ~6.5

CB-5083++++ IC50: 11 nM

Oligomycin A√

Ciclopirox√

Ciclopirox ethanolamine√

Esomeprazole sodium√

BTB06584√

Golgicide A√

Phase 2Phase 4
TOPK

Phase 4Phase 4

HIF-1αPhase 2

CFTR
阻害選択性

Phase 1

Phase 4Phase 4

Inhibitor Name

CFTR

Clinical Phase

VX-809 (Lumacaftor)++++ EC50: 0.1 μM

Phase 3

CFTRinh-172+++

Ki: 300 nM

IOWH032++

IC50: 1.01 μM

GlyH-101+

Ki: 4.3 μM

Ataluren (PTC124)√

Phase 4

Tezacaftor (VX-661)√

Phase 3Phase 2

TRPV

Potassium Channel

阻害選択性

阻害選択性

Inhibitor Name
Potassium Channel

TRAM-34+++

Glimepiride++++ IC50: 3 nM

Gliquidone+++

Vonoprazan Fumarate (TAK-438)++++ IC50: 19 nM

ML133 HCl++

IC50: 290 nM

Gliclazide++

IC50: 184 nM

Other Targets

Clinical Phase

IC50: 27.2 nM++++ IC50: 1 nM-2 nM

Phase 4

GSK2193874+++

IC50: 0.002 μM

Phase 4

SB366791++

IC50: 5.7 nM

Phase 3

Probenecid√

organic anion transport,TAS2R16

Capsazepine√

Na,K-ATPase

Phase 4√√

Amiodarone HCl√

Phase 4

Repaglinide√

Phase 4

Quinine HCl Dihydrate√

Phase 4√Glyburide (Glibenclamide)√

pIC50: 7.1

Phase 4Phase 4Chlorpromazine HCl√

Clinical Phase
Phase 2+

Dofetilide

Dronedarone HCl

Other Targets

AMG-517

Phase 4

Tolbutamide

TRPV

SB705498

Kd: 20 nM

4-Aminopyridine

Dopamine receptor

Phase 4Phase 1
Calcium channel,Sodium channel

Phase 4Phase 4Nateglinide√

Phase 4

Mitiglinide Calcium√

Phase 4CRM1
阻害選択性
Inhibitor Name

CRM1

Selinexor (KPT-330)√

KPT-185√

KPT-276√

Eltanexor (KPT-8602)√

Piperlongumine√

Verdinexor (KPT-335)√

Other Targets

Clinical Phase
Phase 2Phase 2
reactive oxygen species (ROS),PI3K/Akt/mTOR,TrxR1
Phase 1

注釈：

Proton Pump

1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

阻害選択性
Inhibitor Name

Proton Pump

Other Targets

Clinical Phase

Bafilomycin A1(Baf-A1)+++

IC50: 0.44 nM

PF-3716556++

pIC50: ~6.5

Lansoprazole√

Phase 4Omeprazole√

Phase 4NEXIUM (esomeprazole magnesium)√

Phase 4

Zinc Pyrithione√

Dexlansoprazole√

84

Clinical Phase

Clinical Phase

Brefeldin A

Inhibitor Name

Other Targets

Phase 485

Proteases

DPP-4
阻害選択性
E3 Ligase Activators(-)-Parthenolide
NSC 207895
E3 Ligase Antagonists
JNJ-26854165
Thalidomide
Nutlin-3

RING-type E3
E2

E1 Activating Inhibitor
PYR-41

S
C=O

ATP

HECT

=

DUB Inhibitors
PR-619
IU1
P5091
ML323
DegrasynS
C=O

Ub Ub Ub Ub Ub

Ub

DUBs

Ub

DUBs

CDC25CS

G1

Proteasome

DUB Inhibitors
PR-619
IU1
P5091
ML323
Degrasyn

Pan-IκB/IKK Inhibitors
IKK-16
Bardoxolone Methyl
Selective IκB/IKK Inhibitors
TPCA-1 (IKK-2)
IMD 0354 (IKK-2)

NH
C= O

26S Proteasome

Ub Ub

NF-κB Inhibitors
QNZ
Sodium 4-Aminosalicylate
JSH-23SC75741

ATPIκB Kinase
Cellular StressProteasome

CDK–cyclin B
CDK–cyclin A
G0

M
G2

CDK–cyclin A

S

DUBs

Cellular Pathways Associated with the Proteasome

Proteasome

CDC25B

DUBs

S

Ub Ub
Ub Ub

ADP+PiProteasome
WAF1

S
C=O
Ub

Ub RP

Pan-Proteasome Inhibitor
Oprozomib
Selective Proteasome Inhibitors
Bortezomib (20S proteasome)
Carfilzomib (20S proteasome)
MLN9708 (20S proteasome)
ONX-0914 (LMP7)S

E2

HECT-type E3

Ub

AMP+PPiO
Ub C S
E1

RING Finger

E2 Conjugating Inhibitors
NSC697923
BAY 11-7082

CDK–cyclin D

Mdm2 Antagonists
Nutlin-3
Nutlin-3a
YH239-EE
Mdm2 Activator
NSC 207895

CDK–cyclin E

Ub
Ub
Ub

CDC25A, CDC25C
KIP1

ARF
p53
Mdm2

Proteasome

Gene
Expression

Senescencep53
p53

Proteasome Inhibition
Apoptosis

StressApoptosis

p53 Activators
JNJ-26854165
NSC 319726
p53 Inhibitors
Pifithrin-α
Pifithrin-μ

Proteasome Inhibition

Proteasome

詳細情報はP57に記載されています

IκB
Gene
Expression

NF-κB

Proteasome Inhibition

Other Targets

Phase 4Linagliptin++++ IC50: 1 nM

Phase 4

Vildagliptin (LAF-237)+++

IC50: 2.3 nM

Phase 4

Saxagliptin+

IC50: 26 nM

Phase 4

Alogliptin（SYR-322）benzoate++

IC50: <10 nM

Phase 4

Alogliptin+++

IC50: 2.93 nM

Phase 4

Sitagliptin++

IC50: 18 nM

Phase 4Trelagliptin succinate++

IC50: 4 nM

Phase 3Omarigliptin (MK-3102)++++ IC50: 1.6 nM

Teneligliptin hydrobromide+++

Saxagliptin hydrate√

Trelagliptin√

Phase 4

IC50: 1.75 nM

DPP-9

Phase 4IκB NF-κB

Inhibitor Name

HIV Protease

Other Targets

Phase 4++++ Ki: 1.3 pM

Atazanavir Sulfate++

Ki: 2.66 nM

Amprenavir+

IC50: 14.6 ng/mL

Nelfinavir Mesylate+++

Ki: 2 nM

Ritonavir√

Darunavir Ethanolate√

Phase 4

Atazanavir√

Phase 4Limonin√

PXR

Phase 4CYP3A4

詳細情報はP55に記載されています

HCV Protease
阻害選択性

MMP

Batimastat (BB-94)+++

Ilomastat (GM6001, Galardin)++++ Ki: 0.36 nM

SB-3CT+Ki: 13.9 nM

Marimastat (BB-2516)+++

IC50: 5 nM

NSC 405020√

Doxycycline Hyclate√

Nobiletin√

Phase 3Phase 4

Serine Protease+++

EC50: 9 pM-50 pM

Phase 4

Telaprevir (VX-950)++

IC50: 0.35 μM

Phase 4

Lomibuvir (VX-222, VCH-222)+

IC50: 0.94 μM

Phase 2Danoprevir (ITMN-191)++

IC50: 0.2 nM-3.5 nM

Phase 3

Inhibitor Name

Serine Protease

Paritaprevir (ABT-450)+++

EC50: 0.21 nM

Phase 4Gabexate Mesylate++

IC50: 0.19 μM

Grazoprevir++++ Ki: 0.01 nM

Phase 4

Aprotinin+++

Ki: 9.5 nM

Elbasvir√

Phase 4

Alvelestat (AZD9668)++++ IC50: 12 nM

Ombitasvir (ABT-267)√

Phase 4

Nafamostat Mesylate√

Daclatasvir Digydrochloride

√

PMSF

√

Simeprevir√

Phase 4Sivelestat sodium tetrahydrate√

Velpatasvir√

Phase 4Sivelestat (ONO-5046)√

Ledipasvir (GS5885)√

Phase 4

Leupeptin Hemisulfate√

AEBSF HCl√

86

Clinical Phase

IC50: 3 nM

Clinical Phase

Daclatasvir (BMS-790052)

gt1b R155K,gt1b D168V,gt1b D168Y

Phase 4阻害選択性

詳細情報はP36に記載されています

Other Targets

Phase 4

MMP

CaspaseGamma-secretase

HCV Protease

Clinical Phase

Lopinavir

Inhibitor Name

Inhibitor Name

Clinical Phase

IC50: 19 nM

阻害選択性

Pro-survival
Pathway

P

DPP-4
+

HIV ProteaseP

IκB NF-κB

Ub
Ub
Ub

Inhibitor Name
Sitagliptin phosphate monohydrate

阻害選択性
Other Targets

Clinical Phase
Phase 3

Thrombin,Trypsin,kallikrein

Phase 4Phase 2cysteine protease
Phase 4

Cysteine protease87Microbiology

Tyrosinase
阻害選択性
Inhibitor Nametyrosinasemonophenolase

Deoxyarbutin++++ IC50: 50 nM

Kojic acid++

IC50: 0.28 mM

Hexylresorcinol+++

IC50: 0.85 μM

Arbutin+

IC50: 1.09 mM

Monobenzone

√

Aloin

√

diphenolase

Clinical Phase1
Attachment
CCR Antagonist
Maraviroc++

IC50: 1.24 μM+++

2Fusion

IC50: 0.85 μM
Phase 3

Cysteine Protease

13
Maturation
HIV-1

Env
CD4
HIV Protease Inhibitors
Ritonavir
Lopinavir
Atazanavir
Darunavir
Amprenavir
Nelfinavir

Co-receptor (CCR5 or CXCR4)
Uncoating

阻害選択性

Reverse Transcriptase
Inhibitors
Tenofovir (HBV)
Adefovir Dipivoxil (HBV)
Emtricitabine (HIV)Nevirapine (HIV)Rilpivirine (HIV)3

Inhibitor Name

Cysteine Protease

Odanacatib (MK-0822)++++ IC50: 0.2 nM

E-64

+++

IC50: 9 nM

PD 151746+

IC50: 260 nM

Calpeptin++

ID50: 34 nM

Cathepsin Inhibitor 1+++

pIC50: 5.2

PMSF

√

Aloxistatin(E64d)√

Loxistatin Acid (E-64C)√

Leupeptin Hemisulfate√

Z-FA-FMK√

MG-101 (ALLN)√

Other Targets

Clinical Phase
Phase 3CXCR Antagonists
Plerixafor
WZ811

Pre-integration
Complex

Accessory Viral
Proteins
Tat

serine protease

10

8
Nuclear
ExportGag Pol Gag

9Translation

AAA
AAA

6
Integration
LEDGF

ALIX,
ESCRT-I,
ESCRT-III

Assembly

9
TranslationRev

chymotrypsin

Integrase Inhibitors
Raltegravir
Elvitegravir
Dolutegravir
MK-2048
BMS-707035

11
Budding

Gag
Gag Pol

Vif

Vpu

5
NuclearImport4
ReverseTranscription

Host Cell

12
Release

AAA
AAA

CRM1

AAA
AAA
AAA

AAA

AAA

7 Transcription

Phase 3

RNA Pol II
P-TEFb
5’LTR

3’LTR

Glutaminase
阻害選択性
Inhibitor Nameglutaminase

BPTES

++

IC50: 0.16 μM

CB-839+++

IC50: 24 nM

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。

Clinical Phase

HCV Protease

CCR

詳細情報はP86に記載されています

詳細情報はP19に記載されています

Phase 2

HIV Protease

詳細情報はP87に記載されています

2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

Integrase
阻害選択性
Inhibitor Name

88

Integrase

Other Targets

Clinical Phase

Raltegravir (MK-0518)+

IC50: 40 nM

Phase 4

Elvitegravir (GS-9137, JTK-303)++++ IC50: 0.7 nM

Phase 4

Dolutegravir (GSK1349572)+++

IC50: 2.7 nM

Phase 4

BMS-707035++

IC50: 15 nM

Phase 2

MK-2048+++

IC50: 1.5 nM

Phase 1

Dolutegravir Sodium+++

IC50: 2.7 nM

Raltegravir potassium√

Cabotegravir (GSK744, GSK1265744)√

Salicylanilide√

Phase 3Phase 3reverse transcriptase

89

Reverse Transcriptase
阻害選択性
Inhibitor Name

Reverse Transcriptase

Other Targets

Clinical Phase

Didanosine++

IC50: 490 nM

Phase 4

Dapivirine (TMC120)+++

IC50: 24 nM

Phase 3

Tenofovir√

Phase 4

Tenofovir Disoproxil Fumarate√

Phase 4

Emtricitabine√

Phase 4

Entecavir Hydrate√

Adefovir Dipivoxil√

Phase 4

Nevirapine√

Phase 4

Lamivudine√

Phase 4

Stavudine (d4T)√

Phase 4

Telbivudine√

Phase 4Etravirine (TMC125)√

Phase 4

Zidovudine√

Phase 4

Zalcitabine√

Phase 4Abacavir sulfate√

Foscarnet Sodium√

Rilpivirine√

Phase 4

Adefovir√

Phase 4Abacavir√

Phase 4

Efavirenz√

Phase 4

Tenofovir Alafenamide (GS-7340)√

Salicylanilide√

注釈：
1.各阻害剤の半数阻害濃度（IC50）や作用濃度など、詳細についてはwww.selleck.co.jpのウェブサイトをご覧ください。
2.「+」は阻害効果を示す。阻害効果が高い（IC50値が低い）ほど「+」が多く示されている。
3.赤色の「√」は、関連するisoformに対して阻害効果を示すが、特定の値を示さないことを示している。

90

Phase 4
RNA polymerase,DNA polymerase

Phase 4Phase 4integrase