trifarotene [Ligand Id: 9962] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3707313 (Aklief, CD-5789, CD5789, Trifarotene) |
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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 | Activation of RARalpha (unknown origin) expressed in human HeLa cells co-expressing ERE-beta-Glob-Luc-SV-Neo incubated for 18 hrs by luciferase reporter gene assay | B | 6.3 | pKd | 500 | nM | Kd | US-20080015246-A1. Novel ligands that modulate RAR receptors and pharmaceutical/cosmetic compositions comprised thereof (2008) |
| GtoPdb | In a reported assay measuring activation mediated by agonist binding to the RARα ligand-binding domain. | - | 6.3 | pEC50 | 500 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1736-1741 [PMID:29706423] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Activation of RARbeta (unknown origin) expressed in human HeLa cells co-expressing ERE-beta-Glob-Luc-SV-Neo incubated for 18 hrs by luciferase reporter gene assay | B | 7.82 | pKd | 15 | nM | Kd | US-20080015246-A1. Novel ligands that modulate RAR receptors and pharmaceutical/cosmetic compositions comprised thereof (2008) |
| GtoPdb | In a reported assay measuring activation mediated by agonist binding to the RARβ ligand-binding domain. | - | 6.9 | pEC50 | 125 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1736-1741 [PMID:29706423] |
| 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 | 6.9 | pEC50 | 125 | 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] | ||||||||
| ChEMBL | Activation of RARgamma (unknown origin) expressed in human HeLa cells co-expressing ERE-beta-Glob-Luc-SV-Neo incubated for 18 hrs by luciferase reporter gene assay | B | 8.7 | pKd | 2 | nM | Kd | US-20080015246-A1. Novel ligands that modulate RAR receptors and pharmaceutical/cosmetic compositions comprised thereof (2008) |
| GtoPdb | Ligand-induced activation in a cellular reporter assay utlising the RARγ receptor ligand-binding domain. | - | 8.11 | pEC50 | 7.7 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1736-1741 [PMID:29706423] |
| 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 | 8.11 | pEC50 | 7.7 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1736-1741 [PMID:29706423] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
