AGN193109 [Ligand Id: 2640] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL358145
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
ChEMBL Binding affinity towards retinoic acid receptor alpha was determined using [3H]ATRA (5 nM) as radioligand B 7.77 pKd 17 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
ChEMBL Ability to displace 3[H](all-E)-retinoic acid (5 nM) from alpha retinoic acid receptor (alpha RAR) using transactivation assay B 7.8 pKd 16 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 573-576 [PMID:10098666]
ChEMBL Binding constant for baculovirus-expressed Retinoic acid receptor RAR alpha B 8.7 pKd 2 nM Kd J. Med. Chem. (1995) 38: 4764-4767 [PMID:7490725]
ChEMBL Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor alpha F 7.51 pIC50 31 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
GtoPdb - - 8.7 pIC50 - - - J Biol Chem (1996) 271: 22692-6 [PMID:8798442];
J Biol Chem (2000) 275: 19401-8 [PMID:10777502];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Binding affinity towards retinoic acid receptor beta was determined using [3H]ATRA (5 nM) as radioligand B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
ChEMBL Ability to displace 3[H](all-E)-retinoic acid (5 nM) from beta retinoic acid receptor (beta RAR) using transactivation assay B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 573-576 [PMID:10098666]
ChEMBL Binding constant for baculovirus-expressed Retinoic acid receptor RAR beta B 8.7 pKd 2 nM Kd J. Med. Chem. (1995) 38: 4764-4767 [PMID:7490725]
ChEMBL Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor beta F 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
GtoPdb - - 8.7 pIC50 - - - J Biol Chem (1996) 271: 22692-6 [PMID:8798442];
J Biol Chem (2000) 275: 19401-8 [PMID:10777502];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Ability to displace 3[H](all-E)-retinoic acid (5 nM) from Retinoic acid receptor gamma using transactivation assay B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 573-576 [PMID:10098666]
ChEMBL Binding affinity towards retinoic acid receptor gamma was determined using [3H]ATRA (5 nM) as radioligand B 8.22 pKd 6 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
ChEMBL Binding constant for baculovirus-expressed Retinoic acid receptor RAR gamma B 8.52 pKd 3 nM Kd J. Med. Chem. (1995) 38: 4764-4767 [PMID:7490725]
GtoPdb - - 8.5 pIC50 - - - J Biol Chem (1996) 271: 22692-6 [PMID:8798442];
J Biol Chem (2000) 275: 19401-8 [PMID:10777502];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
ChEMBL Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor gamma F 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]