tamibarotene [Ligand Id: 2648] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL25202 (AM80, AM-80, NSC-608000, Tamibarotene)
  • 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 Agonistic activity towards retinoic acid receptor-alpha F 8.19 pKi 6.5 nM Ki J. Med. Chem. (1997) 40: 4222-4234 [PMID:9435893]
GtoPdb - - 6.9 pIC50 - - - J Med Chem (1988) 31: 2182-92 [PMID:3184125];
Mol Cell Biol (1995) 15: 3540-51 [PMID:7791761];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
ChEMBL Binding affinity for Retinoic Acid Receptor alpha (RAR alpha) B 7.11 pIC50 78 nM IC50 J. Med. Chem. (2000) 43: 409-419 [PMID:10669568]
ChEMBL Agonist activity at RARalpha F 7.35 pEC50 45 nM EC50 J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
GtoPdb - - 7.35 pEC50 45 nM EC50 J Med Chem (2010) 53: 6779-810 [PMID:20925433]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Agonistic activity towards retinoic acid receptor-beta F 7.52 pKi 30 nM Ki J. Med. Chem. (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Agonist activity at RARbeta F 6.63 pEC50 235 nM EC50 J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
GtoPdb - - 6.63 pEC50 235 nM EC50 J Med Chem (2010) 53: 6779-810 [PMID:20925433]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Agonist activity at RARgamma F 6.23 pEC50 591 nM EC50 J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
GtoPdb - - 6.23 pEC50 591 nM EC50 J Med Chem (2010) 53: 6779-810 [PMID:20925433]

ChEMBL data shown on this page come from version 28:

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]