AHPN [Ligand Id: 3431] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1180 (O-Demethylated Adapalene)
  • 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 to retinoic acid receptor alpha using [3H]CD 367 as radioligand B 5.19 pKi 6500 nM Ki J. Med. Chem. (1995) 38: 4993-5006 [PMID:8544175]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Binding affinity to retinoic acid receptor beta using [3H]CD 367 as radioligand B 5.61 pKi 2480 nM Ki J. Med. Chem. (1995) 38: 4993-5006 [PMID:8544175]
ChEMBL Agonist activity at GAL4 DNA-binding domain-tagged RARbeta (unknown origin) ligand-binding domain expressed in human HG5LN cells incubated for 18 hrs by luciferase reporter gene assay B 6.65 pEC50 226 nM EC50 Bioorg Med Chem Lett (2018) 28: 1736-1741 [PMID:29706423]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
GtoPdb - - 7.11 pKi 77 nM Ki J Med Chem (1995) 38: 4993-5006 [PMID:8544175]
ChEMBL Binding affinity to retinoic acid receptor (RAR) gamma using [3H]CD 367 as radioligand B 7.11 pKi 77 nM Ki J. Med. Chem. (1995) 38: 4993-5006 [PMID:8544175]
ChEMBL Agonist activity at GAL4 DNA-binding domain-tagged RARgamma (unknown origin) ligand-binding domain expressed in human HG5LN cells incubated for 18 hrs by luciferase reporter gene assay B 7.31 pEC50 49 nM EC50 Bioorg Med Chem Lett (2018) 28: 1736-1741 [PMID:29706423]

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]