dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&gamma;

Ligand: AD5075 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.66 pKi
Reference (Journal): Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects.
Published in: J Biol Chem

Ligand: AD5075 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.66 pKi
Reference (Journal): Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator.
Published in: Mol Endocrinol

Ligand: AD-5061 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone.
Published in: Biochem Biophys Res Commun

Ligand: AD-5061 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes.
Published in: Eur J Pharmacol

Ligand: 15-deoxy-Δ-12,14-prostaglandin J2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Natural ligands of PPARgamma: are prostaglandin J(2) derivatives really playing the part?
Published in: Cell Signal

Ligand: 15-deoxy-Δ-12,14-prostaglandin J2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor gamma and promotes adipocyte differentiation.
Published in: Cell
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&alpha;

Ligand: bezafibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 4.300000190734863 pEC50
Reference (Journal): Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: bezafibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 4.300000190734863 pEC50
Reference (Journal): Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB.
Published in: Biochem Biophys Res Commun

Ligand: AZD4619 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.099999904632568 pEC50
Reference (Webpage): PPAR&alpha; receptor agonist.

Ligand: AD-5061 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone.
Published in: Biochem Biophys Res Commun

Ligand: AD-5061 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes.
Published in: Eur J Pharmacol

Ligand: 8S-HETE (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7 pKd
Reference (Journal): Differential activation of peroxisome proliferator-activated receptors by eicosanoids.
Published in: J Biol Chem

Ligand: 8S-HETE (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7 pKd
Reference (Journal): Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors alpha and delta.
Published in: Proc Natl Acad Sci USA
Target family: 1D. Rev-Erb receptors (type: nhr)
Target: Rev-Erb-&alpha;

Ligand: GSK4112 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.639999866485596 pIC50
Reference (Journal): Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.
Published in: ACS Chem Biol

Ligand: GSK4112 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.
Published in: ACS Chem Biol

Ligand: heme (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways.
Published in: Science

Ligand: heme (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta.
Published in: Nat Struct Mol Biol

Ligand: SR8278 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.
Published in: ACS Chem Biol

Ligand: SR8278 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.
Published in: ACS Chem Biol

Ligand: SR9009 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.170000076293945 pIC50
Reference (Journal): Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
Published in: Nature

Ligand: SR9011 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
Published in: Nature
Target family: 1D. Rev-Erb receptors (type: nhr)
Target: Rev-Erb-&beta;

Ligand: cobalt protoporphyrin IX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.590000152587891 pKd
Reference (Journal): Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist.
Published in: J Biol Chem

Ligand: heme (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.449999809265137 pKd
Reference (Journal): Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist.
Published in: J Biol Chem

Ligand: heme (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.449999809265137 pKd
Reference (Journal): Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways.
Published in: Science

Ligand: heme (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.449999809265137 pKd
Reference (Journal): Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta.
Published in: Nat Struct Mol Biol

Ligand: SR9009 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
Published in: Nature

Ligand: SR9011 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.25 pIC50
Reference (Journal): Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
Published in: Nature

Ligand: zinc protoporphyrin IX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist.
Published in: J Biol Chem
Target family: 1F. Retinoic acid-related orphans (type: nhr)
Target: RAR-related orphan receptor-&alpha;

Ligand: 7-hydroxycholesterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach.
Published in: Anal Biochem

Ligand: CD2314 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.420000076293945 pKd
Reference (Journal): Mechanism of regulation and suppression of melanoma invasiveness by novel retinoic acid receptor-gamma target gene carbohydrate sulfotransferase 10.
Published in: Cancer Res

Ligand: cholesterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha.
Published in: Structure

Ligand: cholesterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): The metastasis suppressor candidate nucleotide diphosphate kinase NM23 specifically interacts with members of the ROR/RZR nuclear orphan receptor subfamily.
Published in: Biochem Biophys Res Commun

Ligand: cholesterol sulphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach.
Published in: Anal Biochem

Ligand: cholesterol sulphate (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha.
Published in: Structure

Ligand: SR1001 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.760000228881836 pKi
Reference (Journal): Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand.
Published in: Nature

Ligand: T0901317 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 6.880000114440918 pKi
Reference (Journal): The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist.
Published in: Mol Pharmacol
Target family: 1F. Retinoic acid-related orphans (type: nhr)
Target: RAR-related orphan receptor-&beta;

Ligand: all-trans-4-oxo-retinoic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: all-trans-4-oxo-retinoic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: ALRT 1550 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: ALRT 1550 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.4 pIC50
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: CD2314 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.840000152587891 pKd
Reference (Journal): Mechanism of regulation and suppression of melanoma invasiveness by novel retinoic acid receptor-gamma target gene carbohydrate sulfotransferase 10.
Published in: Cancer Res

Ligand: tretinoin (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Median affinity: 6.55 pKi
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Median affinity:  -
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol

Ligand: tretinoin (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Median affinity: 9.82 pIC50
Reference (Journal): All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Published in: Nat Struct Biol
Target family: 1H. Liver X receptor-like receptors (type: nhr)
Target: Farnesoid X receptor-&beta;

Ligand: cholesten (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol.
Published in: Mol Cell Biol

Ligand: desmosterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol.
Published in: Mol Cell Biol

Ligand: lanosterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol.
Published in: Mol Cell Biol

Ligand: vitamin D3 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Median affinity: 5 pEC50
Reference (Journal): Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol.
Published in: Mol Cell Biol
Target family: 1I. Vitamin D receptor-like receptors (type: nhr)
Target: Constitutive androstane receptor

Ligand: androstanol (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta.
Published in: Nature
Target family: 1I. Vitamin D receptor-like receptors (type: nhr)
Target: Pregnane X receptor

Ligand: vitamin K2 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Vitamin K2 regulation of bone homeostasis is mediated by the steroid and xenobiotic receptor SXR.
Published in: J Biol Chem

Ligand: trabectedin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007), FDA (2015)
Median affinity: 8.52 pIC50
Reference (Journal): The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux.
Published in: Nat Med

Ligand: SR12813 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution.
Published in: Mol Endocrinol

Ligand: schisandrin A (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.9 pEC50
Reference (Journal): Traditional Chinese medicines Wu Wei Zi (Schisandra chinensis Baill) and Gan Cao (Glycyrrhiza uralensis Fisch) activate pregnane X receptor and increase warfarin clearance in rats.
Published in: J Pharmacol Exp Ther
Target family: 1I. Vitamin D receptor-like receptors (type: nhr)
Target: Constitutive androstane receptor

Ligand: 5β-pregnane-3,20-dione (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.17 pEC50
Reference (Journal): Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands.
Published in: J Biol Chem

Ligand: androstenol (Metabolite)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta.
Published in: Nature

Ligand: CITCO (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes.
Published in: J Biol Chem

Ligand: clotrimazole (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975)
Median affinity: 6.16 pIC50
Reference (Journal): Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands.
Published in: J Biol Chem

Ligand: meclizine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.16 pIC50
Reference (Journal): Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR.
Published in: Mol Endocrinol

Ligand: meclizine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1957)
Median affinity: 7.6 pEC50
Reference (Journal): Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR.
Published in: Mol Endocrinol

Ligand: TCPOBOP (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pEC50
Reference (Journal): The xenobiotic compound 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene is an agonist ligand for the nuclear receptor CAR.
Published in: Mol Cell Biol
Target family: 1.-.-.- Oxidoreductases (type: enzyme)
Target: amine oxidase copper containing 3

Ligand: timolumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Patent): Fully human anti-VAP-1 monoclonal antibodies
Target family: 1.-.-.- Oxidoreductases (type: enzyme)
Target: xanthine dehydrogenase

Ligand: topiroxostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: febuxostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2009)
Primary target: no
Median affinity: 8.899999618530273 pIC50
Reference (Journal): HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.
Published in: Bioorg Med Chem Lett

Ligand: febuxostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2009)
Primary target: yes
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Isocytosine-based inhibitors of xanthine oxidase: design, synthesis, SAR, PK and in vivo efficacy in rat model of hyperuricemia.
Published in: Bioorg Med Chem Lett

Ligand: febuxostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2009)
Primary target: yes
Median affinity: 9.920000076293945 pKi
Reference (Journal): An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition.
Published in: J Biol Chem

Ligand: allopurinol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1966), EMA (2018)
Primary target: yes
Median affinity: 5.380000114440918 pIC50
Reference (Journal): Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase.
Published in: J Med Chem

Ligand: allopurinol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1966), EMA (2018)
Primary target: yes
Median affinity: 5.150000095367432 pKi
Reference (Journal): Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase.
Published in: J Med Chem
Target family: 1.-.-.- Oxidoreductases (type: enzyme)
Target: vitamin K epoxide reductase complex subunit 1

Ligand: warfarin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1954)
Primary target: yes
Median affinity: 5.579999923706055 pKi
Reference (Journal): Determination of the warfarin inhibition constant Ki for vitamin K 2,3-epoxide reductase complex subunit-1 (VKORC1) using an in vitro DTT-driven assay.
Published in: Biochim Biophys Acta

Ligand: phenprocoumon (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1957)
Primary target: yes
Median affinity:  -
Reference (Journal): Effect in man of a new indandione anticoagulant.
Published in: Proc Soc Exp Biol Med

Ligand: phenindione (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (approval date not available)
Primary target: yes
Median affinity:  -
Reference (Journal): Antagonism of anticoagulants dicoumarol, tromexan, and phenylindandione by vitamin K.
Published in: Br Med J

Ligand: phenindione (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (approval date not available)
Primary target: yes
Median affinity:  -
Reference (Journal): Effect in man of a new indandione anticoagulant.
Published in: Proc Soc Exp Biol Med

Ligand: dicumarol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1944)
Primary target: yes
Median affinity:  -
Reference (Journal): Dicoumarol and warfarin.
Published in: Br Heart J

Ligand: alitretinoin (Metabolite)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity:  -
Reference (Journal): VKORC1: a warfarin-sensitive enzyme in vitamin K metabolism and biosynthesis of vitamin K-dependent blood coagulation factors.
Published in: Vitam Horm

Ligand: alitretinoin (Metabolite)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity:  -
Reference (Journal): Pharmacology of warfarin and clinical implications.
Published in: Semin Thromb Hemost

Ligand: acenocoumarol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 6.110000133514404 pIC50
Reference (Journal): Synthesis and structure-activity relationships of novel warfarin derivatives.
Published in: Bioorg Med Chem
Target family: 1.-.-.- Oxidoreductases (type: enzyme)
Target: tyrosinase

Ligand: compound 7 [PMID: 21334791] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.429999828338623 pIC50
Reference (Journal): Synthesis and evaluation of bibenzyl glycosides as potent tyrosinase inhibitors.
Published in: Eur J Med Chem