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ChEMBL ligand: CHEMBL1180 (O-Demethylated Adapalene) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]