dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Protein kinase D (PKD) family (type: enzyme)
Target: protein kinase D2

Ligand: BPKDi (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinase.
Published in: FEBS Lett

Ligand: CRT 0066101 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.600000381469727 pIC50
Reference (Journal): A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
Published in: Mol Cancer Ther
Target family: Protein kinase D (PKD) family (type: enzyme)
Target: protein kinase D3

Ligand: BPKDi (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinase.
Published in: FEBS Lett

Ligand: CRT 0066101 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
Published in: Mol Cancer Ther
Target family: Protein kinase D (PKD) family (type: enzyme)
Target: protein kinase D1

Ligand: kb-NB142-70 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pIC50
Reference (Journal): Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
Published in: ACS Med Chem Lett

Ligand: Gö 6976 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes.
Published in: FEBS Lett

Ligand: CRT 0066101 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
Published in: Mol Cancer Ther

Ligand: compound 13c [PMID: 20684591] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pIC50
Reference (Journal): Identification of orally available naphthyridine protein kinase D inhibitors.
Published in: J Med Chem

Ligand: BPKDi (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinase.
Published in: FEBS Lett
Target family: Protein kinase G (PKG) family (type: enzyme)
Target: Protein kinase G (PKG) 2

Ligand: aplithianine A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.46999979019165 pIC50
Reference (Journal): Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
Published in: J Nat Prod
Target family: Protein kinase G (PKG) family (type: enzyme)
Target: Protein kinase G (PKG) 1

Ligand: allosteric modulator 33 [PMID: 35878399] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.28000020980835 pEC50
Reference (Journal): Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1&#x3b1;.
Published in: J Med Chem

Ligand: aplithianine A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
Published in: J Nat Prod

Ligand: GSK690693 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Published in: J Med Chem

Ligand: ipatasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.159999847412109 pIC50
Reference (Journal): Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
Published in: J Med Chem

Ligand: Rp-8-CPT-cGMPS (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): (Rp)-8-pCPT-cGMPS, a novel cGMP-dependent protein kinase inhibitor.
Published in: Eur J Pharmacol
Target family: Protein kinase G (PKG) family (type: enzyme)
Target: Protein kinase G (PKG) 2

Ligand: compound 32 [PMID: 20471253] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Published in: Bioorg Med Chem Lett
Target family: Protein kinase N (PKN) family (type: enzyme)
Target: protein kinase N2

Ligand: compound 32 [PMID: 20471253] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Published in: Bioorg Med Chem Lett
Target family: Protein kinase N (PKN) family (type: enzyme)
Target: protein kinase N1

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
Published in: J Med Chem

Ligand: RKI-1447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Published in: Medchemcomm
Target family: Protein kinase N (PKN) family (type: enzyme)
Target: protein kinase N2

Ligand: Y27632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pIC50
Reference (Journal): Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Published in: Bioorg Med Chem Lett
Target family: Protein kinase N (PKN) family (type: enzyme)
Target: protein kinase N1

Ligand: compound 20 [PMID: 22136433] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.510000228881836 pIC50
Reference (Journal): 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
Published in: J Med Chem

Ligand: tofacitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2017)
Primary target: no
Median affinity: 6.909999847412109 pIC50
Reference (Journal): Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1).
Published in: Future Med Chem
Target family: Protein phosphatase catalytic subunits (type: enzyme)
Target: protein phosphatase 1 catalytic subunit alpha

Ligand: cantharidin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): The first two cantharidin analogues displaying PP1 selectivity.
Published in: Bioorg Med Chem Lett
Target family: Protein phosphatase catalytic subunits (type: enzyme)
Target: protein phosphatase 2 catalytic subunit alpha

Ligand: okadaic acid (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): The first two cantharidin analogues displaying PP1 selectivity.
Published in: Bioorg Med Chem Lett

Ligand: microcystin-LR (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacokinetic, pharmacodynamic, and behavioural studies of deschloroketamine in Wistar rats.
Published in: Br J Pharmacol

Ligand: cantharidin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): The antiplasmodial activity of norcantharidin analogs.
Published in: Bioorg Med Chem Lett

Ligand: calyculin A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): The first two cantharidin analogues displaying PP1 selectivity.
Published in: Bioorg Med Chem Lett
Target family: Protein phosphatase catalytic subunits (type: enzyme)
Target: protein phosphatase 1 catalytic subunit alpha

Ligand: okadaic acid (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pIC50
Reference (Journal): The first two cantharidin analogues displaying PP1 selectivity.
Published in: Bioorg Med Chem Lett

Ligand: microcystin-LR (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 pIC50
Reference (Journal): Inhibition of the Ser-Thr phosphatases PP1 and PP2A by naturally occurring toxins.
Published in: Bioorg Med Chem

Ligand: calyculin A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): The first two cantharidin analogues displaying PP1 selectivity.
Published in: Bioorg Med Chem Lett
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 1

Ligand: tegeprotafib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Protein tyrosine phosphatase inhibitors and methods of use thereof

Ligand: I-C11 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.929999828338623 pIC50
Reference (Journal): Structure, inhibitor, and regulatory mechanism of Lyp, a lymphoid-specific tyrosine phosphatase implicated in autoimmune diseases.
Published in: Proc Natl Acad Sci USA

Ligand: HPN (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.199999809265137 pIC50
Reference (Journal): HPN, a synthetic analogue of bromophenol from red alga Rhodomela confervoides: synthesis and anti-diabetic effects in C57BL/KsJ-db/db mice.
Published in: Mar Drugs

Ligand: compound 7b [Haftchenary et al., 2013] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.309999942779541 pIC50
Reference (Journal): Identification of a potent salicylic acid-based inhibitor of tyrosine phosphatase PTP1B
Published in: Medchemcomm

Ligand: compound 182 [PMID: 37500611] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.470000267028809 pKi
Reference (Journal): A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.
Published in: Nat Commun

Ligand: compound 182 [PMID: 37500611] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pIC50
Reference (Journal): A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.
Published in: Nat Commun

Ligand: chlorogenic acid (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.960000038146973 pIC50
Reference (Journal): Pyrrolo[1,2-a]quinoxal-5-inium salts and 4,5-dihydropyrrolo[1,2-a]quinoxalines: Synthesis, activity and computational docking for protein tyrosine phosphatase 1B.
Published in: Bioorg Med Chem
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 2

Ligand: compound 182 [PMID: 37500611] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.59000015258789 pKi
Reference (Journal): A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.
Published in: Nat Commun
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 1

Ligand: NC1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pKi
Reference (Journal): Identification and structure-function analyses of an allosteric inhibitor of the tyrosine phosphatase PTPN22.
Published in: J Biol Chem
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 22

Ligand: compound 8a [PMID: 23713581] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pIC50
Reference (Journal): A potent and selective small-molecule inhibitor for the lymphoid-specific tyrosine phosphatase (LYP), a target associated with autoimmune diseases.
Published in: J Med Chem

Ligand: I-C11 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.340000152587891 pIC50
Reference (Journal): Structure, inhibitor, and regulatory mechanism of Lyp, a lymphoid-specific tyrosine phosphatase implicated in autoimmune diseases.
Published in: Proc Natl Acad Sci USA

Ligand: I-C11 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.539999961853027 pKi
Reference (Journal): Structure, inhibitor, and regulatory mechanism of Lyp, a lymphoid-specific tyrosine phosphatase implicated in autoimmune diseases.
Published in: Proc Natl Acad Sci USA

Ligand: NC1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.369999885559082 pKi
Reference (Journal): Identification and structure-function analyses of an allosteric inhibitor of the tyrosine phosphatase PTPN22.
Published in: J Biol Chem
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 2

Ligand: compound 182 [PMID: 37500611] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.239999771118164 pIC50
Reference (Journal): A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.
Published in: Nat Commun
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 11

Ligand: vociprotafib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors

Ligand: migoprotafib (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
Published in: J Med Chem

Ligand: migoprotafib (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pIC50
Reference (Journal): Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
Published in: J Med Chem

Ligand: batoprotafib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.
Published in: J Med Chem
Target family: Protein tyrosine phosphatases non-receptor type (PTPN) (type: enzyme)
Target: protein tyrosine phosphatase non-receptor type 1

Ligand: trodusquemine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice.
Published in: Obesity (Silver Spring)
Target family: Pyrimidine salvage (type: enzyme)
Target: cytidine deaminase

Ligand: cedazuridine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020)
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Design, synthesis, and pharmacological evaluation of fluorinated tetrahydrouridine derivatives as inhibitors of cytidine deaminase.
Published in: J Med Chem
Target family: Pyruvate kinases (EC 2.7.1.40) (type: enzyme)
Target: pyruvate kinase M1/2

Ligand: DMAMCL (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.
Published in: J Med Chem

Ligand: TEPP-46 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Published in: Bioorg Med Chem Lett

Ligand: mitapivat (Synthetic organic)
Interaction type: Allosteric modulator
Action: Activation
Ligand approved: yes
Approval source: EMA & FDA (2022)
Primary target: no
Median affinity: 7 pEC50
Reference (Patent): Therapeutic compounds and compositions

Ligand: DASA-58 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Published in: Bioorg Med Chem Lett

Ligand: compound 24 [PMID: 36723914] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.909999847412109 pIC50
Reference (Journal): Selective Covalent Targeting of Pyruvate Kinase M2 Using Arsenous Warheads.
Published in: J Med Chem

Ligand: compound 1 [PMID: 31465224] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Development of Novel Irreversible Pyruvate Kinase M2 Inhibitors.
Published in: J Med Chem

Ligand: compound 16 [PMID: 31977207] (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pEC50
Reference (Journal): Identification of Parthenolide Dimers as Activators of Pyruvate Kinase M2 in Xenografts of Glioblastoma Multiforme in Vivo.
Published in: J Med Chem
Target family: Pyruvate kinases (EC 2.7.1.40) (type: enzyme)
Target: pyruvate kinase L/R

Ligand: mitapivat (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: EMA & FDA (2022)
Primary target: no
Median affinity:  -
Reference (Journal): AG-348 (Mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes.
Published in: Haematologica

Ligand: etavopivat (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.949999809265137 pEC50
Reference (Journal): Etavopivat, a Pyruvate Kinase Activator in Red Blood Cells, for the Treatment of Sickle Cell Disease.
Published in: J Pharmacol Exp Ther
Target family: QIK subfamily (type: enzyme)
Target: salt inducible kinase 2

Ligand: dasatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2006)
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases.
Published in: Biochem J
Target family: QIK subfamily (type: enzyme)
Target: salt inducible kinase 1

Ligand: ARN-3236 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.670000076293945 pIC50
Reference (Journal): SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype.
Published in: J Leukoc Biol

Ligand: bosutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases.
Published in: Biochem J

Ligand: compound 2c [PMID: 24900538] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.260000228881836 pIC50
Reference (Journal): Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
Published in: ACS Med Chem Lett

Ligand: dasatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2006)
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases.
Published in: Biochem J

Ligand: GLPG3312 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Published in: J Med Chem

Ligand: HG-9-91-01 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.039999961853027 pIC50
Reference (Journal): Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.
Published in: Proc Natl Acad Sci USA