AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: boceprevir
Target: Lysosomal protective protein (Enzyme)
Gene: CTSA
UniProt: P10619 (PPGB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Drug: boceprevir
Target: Cathepsin L2 (Enzyme)
Gene: CTSV
UniProt: O60911 (CATL2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.12
Assay: Inhibition of human Cathepsin V
Drug: boceprevir
Target: Cathepsin K (Enzyme)
Gene: CTSK
UniProt: P43235 (CATK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.4
Assay: Inhibition of human Cathepsin K
Drug: boceprevir
Target: Cathepsin S (Enzyme)
Gene: CTSS
UniProt: P25774 (CATS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.92
Assay: Inhibition of human Cathepsin S
Drug: boceprevir
Target: Cathepsin F (Enzyme)
Gene: CTSF
UniProt: Q9UBX1 (CATF_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.96
Assay: Inhibition of human Cathepsin F
Drug: boceprevir
Target: Hepatitis C virus serine protease, NS3/NS4A (Enzyme)
Gene: NS3|NS4A
UniProt: A3EZI9|D2K2A8 (A3EZI9_9HEPC|D2K2A8_9HEPC)
Organism: Hepatitis C virus
Activity: Ki = 8.959
Action type: INHIBITOR
Assay: Inhibition of HCV 1a NS3/4A protease
Drug: boceprevir
Target: Nonstructural protein NS3-4A (Unclassified)
UniProt: A0A0K1CY61 (A0A0K1CY61_9HEPC)
Organism: Hepatitis C virus
Activity: Ki = 7.85
Drug: telaprevir
Target: Plasminogen (Enzyme)
Gene: PLG
UniProt: P00747 (PLMN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.06
Assay: Inhibition of human plasmin
Drug: telaprevir
Target: Neutrophil elastase (Enzyme)
Gene: ELANE
UniProt: P08246 (ELNE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.17
Assay: Inhibition of human leukocyte elastase after 60 mins fluorescence assay
Drug: telaprevir
Target: Chymotrypsin-like elastase family member 1 (Enzyme)
Gene: CELA1
UniProt: Q9UNI1 (CELA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.52
Assay: Inhibition of human Pancreatic elastase 1
Drug: telaprevir
Target: Cathepsin B (Enzyme)
Gene: CTSB
UniProt: P07858 (CATB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.68
Assay: Inhibition of cathepsin B
Drug: telaprevir
Target: Cathepsin L1 (Enzyme)
Gene: CTSL
UniProt: P07711 (CATL1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.46
Assay: Inhibition of human Cathepsin L
Drug: telaprevir
Target: Chymase (Enzyme)
Gene: CMA1
UniProt: P23946 (CMA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.59
Assay: Inhibition of human Chymase
Drug: telaprevir
Target: Lysosomal protective protein (Enzyme)
Gene: CTSA
UniProt: P10619 (PPGB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Action type: INHIBITOR
Drug: telaprevir
Target: Cathepsin L2 (Enzyme)
Gene: CTSV
UniProt: O60911 (CATL2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.87
Assay: Inhibition of human Cathepsin V
Drug: telaprevir
Target: Cathepsin K (Enzyme)
Gene: CTSK
UniProt: P43235 (CATK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.2
Assay: Inhibition of human Cathepsin K
Drug: telaprevir
Target: Cathepsin S (Enzyme)
Gene: CTSS
UniProt: P25774 (CATS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Assay: Inhibition of human Cathepsin S
Drug: telaprevir
Target: Hepatitis C virus serine protease, NS3/NS4A (Enzyme)
Gene: NS3|NS4A
UniProt: A3EZI9|D2K2A8 (A3EZI9_9HEPC|D2K2A8_9HEPC)
Organism: Hepatitis C virus
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2095231; PROTEIN COMPLEX
Drug: telaprevir
Target: NS3 protease (Unclassified)
UniProt: C1KIQ2 (C1KIQ2_9HEPC)
Organism: Hepacivirus C
Activity: IC50 = 6.89
Assay: Inhibition of HCV genotype 1a NS3 protease V36L mutant expressed in Escherichia coli BL21 (DE3)
Drug: telaprevir
Target: NS3 protease (Unclassified)
Gene: NS3
UniProt: Q0ZMF1 (Q0ZMF1_9HEPC)
Organism: Hepatitis C virus subtype 1b
Activity: Ki = 7.09
Assay: Inhibition of full-length HCV NS3 protease R155K mutant
Drug: telaprevir
Target: NS3 protease (Unclassified)
UniProt: Q91RS4 (Q91RS4_9HEPC)
Organism: Hepacivirus C
Activity: Ki = 8.41
Assay: Inhibition of full-length HCV NS3 protease D168V mutant
Drug: rilpivirine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Assay: Inhibition of human ERG
Drug: rilpivirine
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72547 (Q72547_9HIV1)
Organism: Human immunodeficiency virus 1
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL247; SINGLE PROTEIN
Drug: rilpivirine
Target: Reverse transcriptase (Enzyme)
Gene: reverse transcriptas
UniProt: Q9WKE8 (Q9WKE8_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 7.82
Assay: Inhibition of wild-type HIV-1 reverse transcriptase by fluorescence assay
Drug: rilpivirine
Target: Reverse transcriptase protein (Unclassified)
Gene: reverse transcriptase
UniProt: Q9WJQ2 (Q9WJQ2_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: EC50 = 9.1
Assay: Inhibition of HIV RT K103N/Y181C mutant by cell based assay
Drug: linagliptin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.53
Assay: Displacement of [N-methyl-3H]scopolamine from human recombinant muscarinic M1 receptor expressed in CHO cells
Drug: linagliptin
Target: Dipeptidyl peptidase 4 (Enzyme)
Gene: DPP4
UniProt: P27487 (DPP4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10
Action type: INHIBITOR
Assay: Inhibition of human C-terminal step-tagged DPP4 expressed using baculovirus system
Drug: linagliptin
Target: Prolyl endopeptidase FAP (Enzyme)
Gene: FAP
UniProt: Q12884 (SEPR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.05
Assay: Inhibition of FAPalpha
Drug: linagliptin
Target: Dipeptidyl peptidase 9 (Enzyme)
Gene: DPP9
UniProt: Q86TI2 (DPP9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4
Drug: linagliptin
Target: Prolyl endopeptidase FAP (Enzyme)
Gene: Fap
UniProt: P97321 (SEPR_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.43
Assay: Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition
Drug: linagliptin
Target: Dipeptidyl peptidase IV (Unclassified)
Gene: DPP IV
UniProt: O31048 (O31048_PORGN)
Organism: Porphyromonas gingivalis
Activity: IC50 = 5
Assay: Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate
Drug: abiraterone acetate
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.57
Assay: Inhibition of CYP3A4 expressed in baculovirus infected insect microsomes
Drug: abiraterone acetate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.77
Assay: Antagonist activity at full length human androgen receptor expressed in mammalian expression system measured after 22 to 24 hrs by luciferase reporter gene assay
Drug: abiraterone acetate
Target: Steroid 17-alpha-hydroxylase/17,20 lyase (Enzyme)
Gene: CYP17A1
UniProt: P05093 (CP17A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.54
Action type: INHIBITOR
Assay: Ability to inhibit the C17,20-lyase enzyme by 50% using 17-alpha-hydroxyprogesterone as substrate.
Drug: abiraterone acetate
Target: Cytochrome P450 11B1, mitochondrial (Enzyme)
Gene: CYP11B1
UniProt: P15538 (C11B1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.79
Assay: Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells
Drug: abiraterone acetate
Target: Cytochrome P450 11B2, mitochondrial (Enzyme)
Gene: CYP11B2
UniProt: P19099 (C11B2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.76
Assay: Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells
Drug: abiraterone acetate
Target: Cytochrome P450 17A1 (Enzyme)
Gene: Cyp17a1
UniProt: P11715 (CP17A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.9
Assay: Inhibition of Wistar rat testicular C17,20-lyase using [3H]17-hydroxyprogesterone as substrate preincubated for 20 mins
Drug: gabapentin enacarbil
Target: Voltage-dependent calcium channel subunit alpha-2/delta-1 (Ion channel)
Gene: CACNA2D1
UniProt: P54289 (CA2D1_HUMAN)
Organism: Homo sapiens
Action type: MODULATOR
Assay: Mechanism of Action
Drug: gabapentin enacarbil
Target: Voltage-dependent calcium channel subunit alpha-2/delta-2 (Ion channel)
Gene: CACNA2D2
UniProt: Q9NY47 (CA2D2_HUMAN)
Organism: Homo sapiens
Action type: MODULATOR
Assay: Mechanism of Action
Drug: vandetanib
Target: Macrophage-stimulating protein receptor (Kinase)
Gene: MST1R
UniProt: Q04912 (RON_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.47
Assay: In vitro inhibition of Met proto-oncogene tyrosine kinase (c-Met) expressed in baculovirus
Drug: vandetanib
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.06
Assay: Binding constant for PDGFRB kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase ABL1 (Kinase)
Gene: ABL1
UniProt: P00519 (ABL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.05
Assay: Binding constant for ABL1(Y253F)-phosphorylated kinase domain
Drug: vandetanib
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.47
Assay: Binding constant for KIT(A829P) kinase domain
Drug: vandetanib
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.32
Action type: INHIBITOR
Assay: Binding constant for EGFR(E746-A750del) kinase domain
Drug: vandetanib
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.15
Action type: INHIBITOR
Assay: Binding constant for SRC kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.77
Assay: Binding constant for LCK kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase Yes (Kinase)
Gene: YES1
UniProt: P07947 (YES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.92
Assay: Binding constant for YES kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.44
Assay: Binding constant for FYN kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 2 (Kinase)
Gene: EPHA2
UniProt: P29317 (EPHA2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Action type: INHIBITOR
Assay: Binding constant for EPHA2 kinase domain
Drug: vandetanib
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.72
Assay: Binding constant for FLT3(K663Q) kinase domain
Drug: vandetanib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.85
Action type: INHIBITOR
Assay: Binding constant for RET(M918T) kinase domain
Drug: vandetanib
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.59
Action type: INHIBITOR
Assay: Binding constant for FLT1 kinase domain
Drug: vandetanib
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.33
Action type: INHIBITOR
Assay: Average Binding Constant for VEGFR2; NA=Not Active at 10 uM
Drug: vandetanib
Target: Vascular endothelial growth factor receptor 3 (Kinase)
Gene: FLT4
UniProt: P35916 (VGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.52
Action type: INHIBITOR
Assay: Average Binding Constant for FLT4; NA=Not Active at 10 uM
Drug: vandetanib
Target: Macrophage colony-stimulating factor 1 receptor (Kinase)
Gene: CSF1R
UniProt: P07333 (CSF1R_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for CSF1R kinase domain
Drug: vandetanib
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.64
Assay: Binding constant for PDGFRA kinase domain
Drug: vandetanib
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.59
Action type: INHIBITOR
Assay: Binding constant for ERBB2 kinase domain
Drug: vandetanib
Target: Phosphorylase b kinase gamma catalytic chain, liver/testis isoform (Kinase)
Gene: PHKG2
UniProt: P15735 (PHKG2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.1
Assay: Binding constant for PHKG2 kinase domain
Drug: vandetanib
Target: Fibroblast growth factor receptor 3 (Kinase)
Gene: FGFR3
UniProt: P22607 (FGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Assay: Average Binding Constant for FGFR3; NA=Not Active at 10 uM
Drug: vandetanib
Target: Tyrosine-protein kinase HCK (Kinase)
Gene: HCK
UniProt: P08631 (HCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.44
Assay: Binding constant for HCK kinase domain
Drug: vandetanib
Target: Receptor tyrosine-protein kinase erbB-4 (Kinase)
Gene: ERBB4
UniProt: Q15303 (ERBB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.32
Action type: INHIBITOR
Assay: Binding constant for ERBB4 kinase domain
Drug: vandetanib
Target: Rho-associated protein kinase 2 (Kinase)
Gene: ROCK2
UniProt: O75116 (ROCK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.44
Assay: Binding constant for ROCK2 kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase CSK (Kinase)
Gene: CSK
UniProt: P41240 (CSK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.6
Assay: Binding constant for full-length CSK
Drug: vandetanib
Target: Angiopoietin-1 receptor (Kinase)
Gene: TEK
UniProt: Q02763 (TIE2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Action type: INHIBITOR
Assay: Binding constant for TIE2 kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 8 (Kinase)
Gene: EPHA8
UniProt: P29322 (EPHA8_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.04
Action type: INHIBITOR
Assay: Binding constant for EPHA8 kinase domain
Drug: vandetanib
Target: Hepatocyte growth factor receptor (Kinase)
Gene: MET
UniProt: P08581 (MET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.39
Assay: Binding constant for MET(Y1235D) kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase Lyn (Kinase)
Gene: LYN
UniProt: P07948 (LYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.96
Assay: Binding constant for LYN kinase domain
Drug: vandetanib
Target: 5'-AMP-activated protein kinase catalytic subunit alpha-1 (Kinase)
Gene: PRKAA1
UniProt: Q13131 (AAPK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.52
Assay: Binding constant for AMPK-alpha1 kinase domain
Drug: vandetanib
Target: Fibroblast growth factor receptor 1 (Kinase)
Gene: FGFR1
UniProt: P11362 (FGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.25
Assay: Binding constant for FGFR1 kinase domain
Drug: vandetanib
Target: Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (Kinase)
Gene: PHKG1
UniProt: Q16816 (PHKG1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for full-length PHKG1
Drug: vandetanib
Target: Serine/threonine-protein kinase 10 (Kinase)
Gene: STK10
UniProt: O94804 (STK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.09
Assay: Binding constant for LOK kinase domain
Drug: vandetanib
Target: Serine/threonine-protein kinase PLK4 (Kinase)
Gene: PLK4
UniProt: O00444 (PLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.21
Assay: Binding constant for PLK4 kinase domain
Drug: vandetanib
Target: Aurora kinase C (Kinase)
Gene: AURKC
UniProt: Q9UQB9 (AURKC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.82
Assay: Binding constant for full-length AURKC
Drug: vandetanib
Target: Abelson tyrosine-protein kinase 2 (Kinase)
Gene: ABL2
UniProt: P42684 (ABL2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.16
Assay: Binding constant for ABL2 kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 5 (Kinase)
Gene: EPHA5
UniProt: P54756 (EPHA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Action type: INHIBITOR
Assay: Binding constant for EPHA5 kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 4 (Kinase)
Gene: EPHA4
UniProt: P54764 (EPHA4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Action type: INHIBITOR
Assay: Binding constant for EPHA4 kinase domain
Drug: vandetanib
Target: Fibroblast growth factor receptor 2 (Kinase)
Gene: FGFR2
UniProt: P21802 (FGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for FGFR2 kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 6 (Kinase)
Gene: EPHA6
UniProt: Q9UF33 (EPHA6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.3
Action type: INHIBITOR
Assay: Binding constant for EPHA6 kinase domain
Drug: vandetanib
Target: TRAF2 and NCK-interacting protein kinase (Kinase)
Gene: TNIK
UniProt: Q9UKE5 (TNIK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.64
Assay: Binding constant for TNIK kinase domain
Drug: vandetanib
Target: Casein kinase I isoform epsilon (Kinase)
Gene: CSNK1E
UniProt: P49674 (KC1E_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.82
Assay: Average Binding Constant for CSNK1E; NA=Not Active at 10 uM
Drug: vandetanib
Target: Tyrosine-protein kinase Fgr (Kinase)
Gene: FGR
UniProt: P09769 (FGR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.57
Assay: Binding constant for FGR kinase domain
Drug: vandetanib
Target: ALK tyrosine kinase receptor (Kinase)
Gene: ALK
UniProt: Q9UM73 (ALK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for ALK kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 3 (Kinase)
Gene: EPHA3
UniProt: P29320 (EPHA3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Action type: INHIBITOR
Assay: Average Binding Constant for EPHA3; NA=Not Active at 10 uM
Drug: vandetanib
Target: Tyrosine-protein kinase FRK (Kinase)
Gene: FRK
UniProt: P42685 (FRK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.77
Assay: Binding constant for FRK kinase domain
Drug: vandetanib
Target: Mitogen-activated protein kinase kinase kinase kinase 5 (Kinase)
Gene: MAP4K5
UniProt: Q9Y4K4 (M4K5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.35
Assay: Binding constant for MAP4K5 kinase domain
Drug: vandetanib
Target: Mitogen-activated protein kinase kinase kinase 4 (Kinase)
Gene: MAP3K4
UniProt: Q9Y6R4 (M3K4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.52
Assay: Binding constant for MAP3K4 kinase domain
Drug: vandetanib
Target: Cyclin-G-associated kinase (Kinase)
Gene: GAK
UniProt: O14976 (GAK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.07
Assay: Binding constant for GAK kinase domain
Drug: vandetanib
Target: Receptor-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: RIPK2
UniProt: O43353 (RIPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.34
Assay: Binding constant for RIPK2 kinase domain
Drug: vandetanib
Target: Ephrin type-B receptor 1 (Kinase)
Gene: EPHB1
UniProt: P54762 (EPHB1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.54
Action type: INHIBITOR
Assay: Binding constant for EPHB1 kinase domain
Drug: vandetanib
Target: Ephrin type-A receptor 7 (Kinase)
Gene: EPHA7
UniProt: Q15375 (EPHA7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.62
Action type: INHIBITOR
Assay: Binding constant for EPHA7 kinase domain
Drug: vandetanib
Target: STE20-like serine/threonine-protein kinase (Kinase)
Gene: SLK
UniProt: Q9H2G2 (SLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.02
Assay: Average Binding Constant for SLK; NA=Not Active at 10 uM
Drug: vandetanib
Target: MAP kinase-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: MKNK2
UniProt: Q9HBH9 (MKNK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.77
Assay: Binding constant for MKNK2 kinase domain
Drug: vandetanib
Target: Epithelial discoidin domain-containing receptor 1 (Kinase)
Gene: DDR1
UniProt: Q08345 (DDR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.96
Assay: Binding constant for DDR1 kinase domain
Drug: vandetanib
Target: Ephrin type-B receptor 4 (Kinase)
Gene: EPHB4
UniProt: P54760 (EPHB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Action type: INHIBITOR
Assay: Binding constant for EPHB4 kinase domain
Drug: vandetanib
Target: Serine/threonine-protein kinase receptor R3 (Kinase)
Gene: ACVRL1
UniProt: P37023 (ACVL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.33
Assay: Binding constant for ACVRL1 kinase domain
Drug: vandetanib
Target: Activin receptor type-1 (Kinase)
Gene: ACVR1
UniProt: Q04771 (ACVR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.82
Assay: Binding constant for ACVR1 kinase domain
Drug: vandetanib
Target: Dual specificity mitogen-activated protein kinase kinase 1 (Kinase)
Gene: MAP2K1
UniProt: Q02750 (MP2K1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Assay: Binding constant for full-length MEK1
Drug: vandetanib
Target: Dual specificity mitogen-activated protein kinase kinase 2 (Kinase)
Gene: MAP2K2
UniProt: P36507 (MP2K2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for full-length MEK2
Drug: vandetanib
Target: Protein-tyrosine kinase 6 (Kinase)
Gene: PTK6
UniProt: Q13882 (PTK6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.48
Action type: INHIBITOR
Assay: Average Binding Constant for PTK6; NA=Not Active at 10 uM
Drug: vandetanib
Target: Tyrosine-protein kinase BTK (Kinase)
Gene: BTK
UniProt: Q06187 (BTK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.77
Assay: Binding constant for BTK kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase receptor UFO (Kinase)
Gene: AXL
UniProt: P30530 (UFO_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.6
Assay: Binding constant for AXL kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase receptor TYRO3 (Kinase)
Gene: TYRO3
UniProt: Q06418 (TYRO3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.03
Assay: Binding constant for TYRO3 kinase domain
Drug: vandetanib
Target: Ephrin type-B receptor 2 (Kinase)
Gene: EPHB2
UniProt: P29323 (EPHB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.36
Action type: INHIBITOR
Assay: Binding constant for EPHB2 kinase domain
Drug: vandetanib
Target: Cyclin-dependent kinase 7 (Kinase)
Gene: CDK7
UniProt: P50613 (CDK7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.39
Assay: Binding constant for CDK7 kinase domain
Drug: vandetanib
Target: Ribosomal protein S6 kinase beta-1 (Kinase)
Gene: RPS6KB1
UniProt: P23443 (KS6B1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.8
Assay: Binding constant for S6K1 kinase domain
Drug: vandetanib
Target: Ribosomal protein S6 kinase alpha-6 (Kinase)
Gene: RPS6KA6
UniProt: Q9UK32 (KS6A6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.62
Assay: Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain
Drug: vandetanib
Target: Mitogen-activated protein kinase kinase kinase MLT (Kinase)
Gene: ZAK
UniProt: Q9NYL2 (MLTK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.29
Assay: Binding constant for ZAK kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase receptor Tie-1 (Kinase)
Gene: TIE1
UniProt: P35590 (TIE1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.82
Assay: Binding constant for TIE1 kinase domain
Drug: vandetanib
Target: Tyrosine-protein kinase TXK (Kinase)
Gene: TXK
UniProt: P42681 (TXK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.43
Assay: Binding constant for TXK kinase domain
Drug: vandetanib
Target: MAP kinase-interacting serine/threonine-protein kinase 1 (Kinase)
Gene: MKNK1
UniProt: Q9BUB5 (MKNK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.44
Assay: Binding constant for full-length MKNK1
Drug: vandetanib
Target: Serine/threonine-protein kinase SIK2 (Kinase)
Gene: SIK2
UniProt: Q9H0K1 (SIK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.37
Assay: Binding constant for full-length SNF1LK2
Drug: vandetanib
Target: Serine/threonine-protein kinase 33 (Kinase)
Gene: STK33
UniProt: Q9BYT3 (STK33_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.85
Assay: Binding constant for full-length STK33
Drug: vandetanib
Target: Serine/threonine-protein kinase TNNI3K (Kinase)
Gene: TNNI3K
UniProt: Q59H18 (TNI3K_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.55
Assay: Binding constant for full-length TNNI3K
Drug: vandetanib
Target: Discoidin domain-containing receptor 2 (Kinase)
Gene: DDR2
UniProt: Q16832 (DDR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.49
Assay: Binding constant for DDR2 kinase domain