tamibarotene [Ligand Id: 2648] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL25202 (Am80, AM-80, Amnoid, INNO-507, NSC-608000, OP-01, RR-110, Sy-1425, SY-1425, Tamibarotene, Tamibaroteno, TM-411, TOS-80T) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Flavin reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5019] [UniProtKB: P30043] | ||||||||
| ChEMBL | Binding affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry | B | 5.86 | pKd | 1380.38 | nM | Kd | J Med Chem (2022) 65: 2548-2557 [PMID:34957824] |
| ChEMBL | Binding affinity to human N-terminal His6-tagged and thrombin cleavage fused BLVRB expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry | B | 5.86 | pKd | 1380 | nM | Kd | J Med Chem (2022) 65: 2548-2557 [PMID:34957824] |
| 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 35:
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]
