dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: 2.3.1.-  Acyltransferases (type: enzyme)
Target: diacylglycerol O-acyltransferase 1

Ligand: T863 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor.
Published in: J Med Chem

Ligand: PF-04620110 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 pIC50
Reference (Journal): Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Published in: ACS Med Chem Lett

Ligand: compound 5B [PMID: 25349648] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.40999984741211 pIC50
Reference (Journal): Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.
Published in: ACS Med Chem Lett

Ligand: compound 23n [PMID: 24900877] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.190000057220459 pIC50
Reference (Journal): Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
Published in: ACS Med Chem Lett

Ligand: AZD7687 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Published in: J Med Chem
Target family: 2.3.1.-  Acyltransferases (type: enzyme)
Target: monoacylglycerol O-acyltransferase 2

Ligand: BMS-986172 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Discovery of <b>12</b> (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders.
Published in: J Med Chem

Ligand: BMS-986172 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.34000015258789 pIC50
Reference (Journal): Discovery of <b>12</b> (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders.
Published in: J Med Chem
Target family: 2.3.1.-  Acyltransferases (type: enzyme)
Target: N-acetyltransferase 8 like

Ligand: compound 5 [Stecula et al., 2020] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pKi
Reference (Journal): Discovery of Novel Inhibitors of a Critical Brain Enzyme Using a Homology Model and a Deep Convolutional Neural Network
Published in: Journal of Medicinal Chemistry
Target family: 2.3.1.-  Acyltransferases (type: enzyme)
Target: monoacylglycerol O-acyltransferase 2

Ligand: BMS-963272 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Published in: J Med Chem
Target family: 2.3.1.-  Acyltransferases (type: enzyme)
Target: zinc finger DHHC-type palmitoyltransferase 3

Ligand: benzosceptrin C (Natural product)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.409999847412109 pKd
Reference (Journal): Benzosceptrin C induces lysosomal degradation of PD-L1 and promotes antitumor immunity by targeting DHHC3.
Published in: Cell Rep Med
Target family: 2.3.1.-  Acyltransferases (type: enzyme)
Target: monoacylglycerol O-acyltransferase 2

Ligand: BMS-963272 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Published in: J Med Chem
Target family: 2.3.2.13 Transglutaminases (type: enzyme)
Target: transglutaminase 2

Ligand: compound 11 [PMID: 37449845] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.159999847412109 pKd
Reference (Journal): Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2).
Published in: J Med Chem

Ligand: ERW1041E (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Characterization of Transglutaminase 2 activity inhibitors in monocytes in vitro and their effect in a mouse model for multiple sclerosis.
Published in: PLoS ONE

Ligand: JAK3 inhibitor IV (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.
Published in: Chem Biol

Ligand: ZED1227 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.28000020980835 pIC50
Reference (Journal): Features of ZED1227: The First-In-Class Tissue Transglutaminase Inhibitor Undergoing Clinical Evaluation for the Treatment of Celiac Disease.
Published in: Cells
Target family: 2.4.2.1 Purine-nucleoside phosphorylase (type: enzyme)
Target: purine nucleoside phosphorylase

Ligand: forodesine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.140000343322754 pKi
Reference (Journal): One-third-the-sites transition-state inhibitors for purine nucleoside phosphorylase.
Published in: Biochemistry
Target family: 2.5.1.18 Glutathione transferases (type: enzyme)
Target: glutathione S-transferase omega 1

Ligand: C1-27 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors.
Published in: J Med Chem

Ligand: compound 25 [PMID: 32105470] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors.
Published in: J Med Chem
Target family: 2.5.1.58 Protein farnesyltransferase (type: enzyme)
Target: farnesyltransferase, CAAX box, subunit beta

Ligand: LB42908 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase).
Published in: Bioorg Med Chem Lett

Ligand: BMS-214662 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.869999885559082 pIC50
Reference (Journal): Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
Published in: J Med Chem

Ligand: FTI 276 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes.
Published in: J Biol Chem

Ligand: L-739,750 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.739999771118164 pIC50
Reference (Journal): Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice.
Published in: Proc Natl Acad Sci USA

Ligand: tipifarnib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.069999694824219 pIC50
Reference (Journal): Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.
Published in: Cancer Res

Ligand: tipifarnib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.069999694824219 pIC50
Reference (Journal): 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.
Published in: Bioorg Med Chem Lett
Target family: 2.6.1.42 Branched-chain-amino-acid transaminase (type: enzyme)
Target: branched chain amino acid transaminase 2

Ligand: BAY-069 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pIC50
Reference (Journal): BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe.
Published in: J Med Chem

Ligand: compound 27 [PMID: 26938474] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.
Published in: J Med Chem

Ligand: compound 42 [PMID: 26938474] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.
Published in: J Med Chem
Target family: 2.6.1.42 Branched-chain-amino-acid transaminase (type: enzyme)
Target: branched chain amino acid transaminase 1

Ligand: BAY-069 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe.
Published in: J Med Chem
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: monoacylglycerol lipase

Ligand: KML29 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates.
Published in: Chem Biol
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: &alpha;&beta;-Hydrolase 12

Ligand: DO264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12).
Published in: J Med Chem
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: monoacylglycerol lipase

Ligand: ABD-1970 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.
Published in: J Pharmacol Exp Ther
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: &alpha;&beta;-Hydrolase 12

Ligand: orlistat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999), EMA (1998)
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling.
Published in: Bioorg Med Chem Lett
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: &alpha;&beta;-Hydrolase 6

Ligand: ABD-1970 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.
Published in: J Pharmacol Exp Ther

Ligand: ABD-1970 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.489999771118164 pIC50
Reference (Journal): Monoacylglycerol Lipase Inhibition in Human and Rodent Systems Supports Clinical Evaluation of Endocannabinoid Modulators.
Published in: J Pharmacol Exp Ther

Ligand: ABX-1431 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.570000171661377 pIC50
Reference (Journal): Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.
Published in: J Med Chem

Ligand: KT-109 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses.
Published in: Nat Chem Biol

Ligand: SA-57 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.190000057220459 pIC50
Reference (Journal): O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors.
Published in: ACS Chem Neurosci

Ligand: WWL123 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening.
Published in: Proc Natl Acad Sci USA

Ligand: WWL70 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases.
Published in: J Am Chem Soc
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: diacylglycerol lipase &alpha;

Ligand: DH376 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pIC50
Reference (Journal): Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding.
Published in: J Med Chem

Ligand: DH376 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition.
Published in: Proc Natl Acad Sci USA

Ligand: DO34 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition.
Published in: Proc Natl Acad Sci USA

Ligand: KT-109 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.639999866485596 pIC50
Reference (Journal): DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses.
Published in: Nat Chem Biol

Ligand: LEI105 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons.
Published in: J Am Chem Soc

Ligand: LEI105 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons.
Published in: J Am Chem Soc

Ligand: orlistat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999), EMA (1998)
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain.
Published in: J Cell Biol

Ligand: RHC80267 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.190000057220459 pIC50
Reference (Journal): Assay and inhibition of diacylglycerol lipase activity.
Published in: Bioorg Med Chem Lett
Target family: 2-Acylglycerol ester turnover (type: enzyme)
Target: diacylglycerol lipase &beta;

Ligand: DH376 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition.
Published in: Proc Natl Acad Sci USA

Ligand: DO34 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition.
Published in: Proc Natl Acad Sci USA

Ligand: KT-109 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses.
Published in: Nat Chem Biol

Ligand: KT-109 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.090000152587891 pIC50
Reference (Journal): DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses.
Published in: Nat Chem Biol

Ligand: LEI105 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons.
Published in: J Am Chem Soc

Ligand: orlistat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999), EMA (1998)
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain.
Published in: J Cell Biol

Ligand: RHC80267 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: 2A. Hepatocyte nuclear factor-4 receptors (type: nhr)
Target: Hepatocyte nuclear factor-4-&alpha;

Ligand: linoleic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Identification of an endogenous ligand bound to a native orphan nuclear receptor.
Published in: PLoS ONE

Ligand: BI6015 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter.
Published in: Chem Biol
Target family: 2B. Retinoid X receptors (type: nhr)
Target: Retinoid X receptor-&alpha;

Ligand: AGN194204 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes.
Published in: J Med Chem
Target family: 2B. Retinoid X receptors (type: nhr)
Target: Retinoid X receptor-&beta;

Ligand: LG100754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands.
Published in: J Biol Chem

Ligand: LG100754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Activation of specific RXR heterodimers by an antagonist of RXR homodimers.
Published in: Nature

Ligand: LG100754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo.
Published in: Mol Endocrinol

Ligand: LG100268 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Activation of specific RXR heterodimers by an antagonist of RXR homodimers.
Published in: Nature

Ligand: LG100268 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties.
Published in: J Med Chem
Target family: 2B. Retinoid X receptors (type: nhr)
Target: Retinoid X receptor-&beta;

Ligand: UVI3003 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers.
Published in: J Med Chem

Ligand: [3H]9-cis-retinoic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKd
Reference (Journal): Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids.
Published in: Proc Natl Acad Sci USA
Target family: 2C. Testicular receptors (type: nhr)
Target: Testicular receptor 4

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity: 4.619999885559082 pEC50
Reference (Journal): The orphan nuclear receptor TR4 is a vitamin A-activated nuclear receptor.
Published in: J Biol Chem

Ligand: retinol (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 4.710000038146973 pEC50
Reference (Journal): The orphan nuclear receptor TR4 is a vitamin A-activated nuclear receptor.
Published in: J Biol Chem