trifarotene [Ligand Id: 9962] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3707313 (Aklief, CD-5789, CD5789, Trifarotene, Trifaroteno) |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
