dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Prolyl hydroxylases (type: enzyme)
Target: egl-9 family hypoxia inducible factor 1

Ligand: compound 6ee [PMID: 22364528] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): 1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Published in: J Med Chem

Ligand: DDO-3055 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.190000057220459 pIC50
Reference (Journal): Discovery of Clinical Candidate (5-(3-(4-Chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an Orally Bioavailable Prolyl Hydroxylase Inhibitor for the Treatment of Anemia.
Published in: J Med Chem

Ligand: enarodustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 6.659999847412109 pIC50
Reference (Journal): Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.
Published in: ACS Med Chem Lett

Ligand: IOX1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.480000019073486 pIC50
Reference (Journal): A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1.
Published in: ChemMedChem

Ligand: IOX2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases.
Published in: ACS Chem Biol

Ligand: vadadustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020), EMA (2023), FDA (2024)
Primary target: no
Median affinity: 7.539999961853027 pIC50
Reference (Journal): Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.
Published in: Chem Sci
Target family: Prostaglandin synthases (type: enzyme)
Target: CYP8A1

Ligand: compound 7p [PMID: 7861416] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids.
Published in: J Med Chem
Target family: Prostaglandin synthases (type: enzyme)
Target: AKR1C3

Ligand: compound 1 [Lolli et al., 2019] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3.
Published in: ACS Med Chem Lett

Ligand: KV-37 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): AKR1C3 Inhibitor KV-37 Exhibits Antineoplastic Effects and Potentiates Enzalutamide in Combination Therapy in Prostate Adenocarcinoma Cells.
Published in: Mol Cancer Ther

Ligand: tolfenamic acid (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: UK (1997)
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase.
Published in: J Biol Chem
Target family: Prostaglandin synthases (type: enzyme)
Target: CBR1

Ligand: wedelolactone (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.420000076293945 pIC50
Reference (Journal): Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone.
Published in: Bioorg Med Chem
Target family: Prostaglandin synthases (type: enzyme)
Target: CYP5A1

Ligand: camonagrel (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The mechanism of anti-thrombotic, thrombolytic and fibrinolytic actions of camonagrel--a new thromboxane synthase inhibitor.
Published in: Wien Klin Wochenschr

Ligand: compound 10a [PMID: 1447738] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
Published in: J Med Chem

Ligand: compound 7p [PMID: 7861416] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids.
Published in: J Med Chem

Ligand: dazoxiben (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): UK-37, 248, a novel, selective thromboxane synthetase inhibitor with platelet anti-aggregatory and anti-thrombotic activity.
Published in: Thromb Res

Ligand: furegrelate sodium (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate.
Published in: Prostaglandins

Ligand: ozagrel (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China and Japan only
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase.
Published in: J Med Chem

Ligand: ozagrel (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China and Japan only
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Pharmacological studies on the TXA2 synthetase inhibitor (E)-3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propenoic acid (OKY-046).
Published in: Jpn J Pharmacol
Target family: Prostaglandin synthases (type: enzyme)
Target: mPGES2

Ligand: compound 30 [PMID: 15953724] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.
Published in: Bioorg Med Chem Lett
Target family: Prostaglandin synthases (type: enzyme)
Target: mPGES1

Ligand: compound 30 [PMID: 15953724] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.
Published in: Bioorg Med Chem Lett
Target family: Prostaglandin synthases (type: enzyme)
Target: L-PGDS

Ligand: AT-56 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.119999885559082 pKi
Reference (Journal): Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase.
Published in: J Biol Chem
Target family: Prostaglandin synthases (type: enzyme)
Target: H-PGDS

Ligand: TFC007 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.079999923706055 pIC50
Reference (Journal): Inhibition of hematopoietic prostaglandin D synthase improves allergic nasal blockage in guinea pigs.
Published in: Prostaglandins Other Lipid Mediat
Target family: Prostaglandin synthases (type: enzyme)
Target: mPGES1

Ligand: zaloglanstat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Patent): Mpges-1 inhibitor for the treatment of osteoarthritis pain
Target family: Prostaglandin synthases (type: enzyme)
Target: H-PGDS

Ligand: HQL-79 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Structural and functional characterization of HQL-79, an orally selective inhibitor of human hematopoietic prostaglandin D synthase.
Published in: J Biol Chem
Target family: Prostaglandin synthases (type: enzyme)
Target: HPGD

Ligand: compound 3 [PMID: 21650226] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors.
Published in: J Med Chem
Target family: Prostaglandin synthases (type: enzyme)
Target: CYP8A1

Ligand: tranylcypromine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Primary target: no
Median affinity:  -
Reference (Journal): Arterial walls are protected against deposition of platelet thrombi by a substance (prostaglandin X) which they make from prostaglandin endoperoxides.
Published in: Prostaglandins
Target family: Prostaglandin synthases (type: enzyme)
Target: CYP5A1

Ligand: picotamide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.799999952316284 pIC50
Reference (Journal): Characterization of N,N'-bis(3-picolyl)-4-methoxy-isophtalamide (picotamide) as a dual thromboxane synthase inhibitor/thromboxane A2 receptor antagonist in human platelets.
Published in: Thromb Haemost
Target family: Prostanoid receptors (type: gpcr)
Target: EP<sub>4</sub> receptor

Ligand: 19(R)-OH-PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol
Target family: Prostanoid receptors (type: gpcr)
Target: EP<sub>4</sub> receptor

Ligand: 11-deoxy-PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: 11-deoxy-PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: 11-deoxy-PGE1 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.33 pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

Ligand: 11-deoxy-PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Median affinity: 9 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: 13,14-dihydro-PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: 16,16-dimethyl-PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: 17-phenyl-ω-trinor-PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The EP1/EP3 receptor agonist 17-pt-PGE<sub>2</sub> acts as an EP4 receptor agonist on endothelial barrier function and in a model of LPS-induced pulmonary inflammation.
Published in: Vascul Pharmacol
Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR2

Ligand: AC264613 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): Discovery of potent and selective small-molecule PAR-2 agonists.
Published in: J Med Chem
Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR4

Ligand: GYPGKF-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: GYPGQV-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: ML354 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Published in: Bioorg Med Chem Lett

Ligand: P4pal-10 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation.
Published in: Nat Med

Ligand: RAG8 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Targeting a Proteinase-Activated Receptor 4 (PAR4) Carboxyl Terminal Motif to Regulate Platelet Function.
Published in: Mol Pharmacol

Ligand: UDM-001651 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pIC50
Reference (Journal): Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.
Published in: J Med Chem

Ligand: YD-3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Published in: Bioorg Med Chem Lett
Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR4

Ligand: AYPGKF-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: BMS-986120 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Published in: J Med Chem

Ligand: BMS-986120 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.
Published in: Sci Transl Med

Ligand: BMS-986141 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Published in: J Med Chem
Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR2

Ligand: 2-furoyl-LIGRLO-amide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist.
Published in: J Pharmacol Exp Ther

Ligand: 2-furoyl-LIGRL[N[3H]propionyl]-O-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: binding and visualization.
Published in: J Pharmacol Exp Ther

Ligand: 2-furoyl-LIGRL[N-(Alexa Fluor 594)-O]-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: binding and visualization.
Published in: J Pharmacol Exp Ther
Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR1

Ligand: vorapaxar (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: yes
Median affinity: 8.09000015258789 pKi
Reference (Journal): Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Published in: J Med Chem

Ligand: TFLLR-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.409999847412109 pEC50
Reference (Journal): Proteinase-activated receptors: structural requirements for activity, receptor cross-reactivity, and receptor selectivity of receptor-activating peptides.
Published in: Can J Physiol Pharmacol

Ligand: [3H]haTRAP (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.82 pKd
Reference (Journal): Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor.
Published in: Mol Pharmacol

Ligand: SCH-79797 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pIC50
Reference (Journal): Inhibition of cellular action of thrombin by N3-cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist.
Published in: Biochem Pharmacol

Ligand: RWJ-56110 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.360000133514404 pIC50
Reference (Journal): Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor.
Published in: Proc Natl Acad Sci USA

Ligand: F16357 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.190000057220459 pIC50

Ligand: atopaxar (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.72 pIC50
Reference (Journal): The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs.
Published in: Eur J Pharmacol
Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR2

Ligand: [3H]2-furoyl-LIGRL-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2.
Published in: Br J Pharmacol

Ligand: SLIGRL-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Proteinase-activated receptor-1 (PAR(1)) and PAR(2) but not PAR(4) mediate contraction in human and guinea-pig gallbladders.
Published in: Neurogastroenterol Motil

Ligand: SLIGKV-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Proteinase-activated receptor-1 (PAR(1)) and PAR(2) but not PAR(4) mediate contraction in human and guinea-pig gallbladders.
Published in: Neurogastroenterol Motil
Target family: Protein kinase A (PKA) family (type: enzyme)
Target: protein kinase, cAMP-dependent, catalytic, alpha subunit

Ligand: aplithianine A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.079999923706055 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: 7.71999979019165 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: H-89 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.320000171661377 pKi
Reference (Journal): Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells.
Published in: J Biol Chem

Ligand: ripasudil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 5.679999828338623 pIC50
Reference (Journal): Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits.
Published in: Curr Eye Res
Target family: Protein kinase A (PKA) family (type: enzyme)
Target: protein kinase, cAMP-dependent, catalytic, beta subunit

Ligand: GSK690693 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): The synthesis and evaluation of indolylureas as PKCα inhibitors.
Published in: Bioorg Med Chem
Target family: Protein kinase A (PKA) family (type: enzyme)
Target: protein kinase X-linked

Ligand: GSK690693 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 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
Target family: Protein kinase D (PKD) family (type: enzyme)
Target: protein kinase D1

Ligand: NIK SMI1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pKi
Reference (Journal): NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.
Published in: Nat Commun