LG100754 [Ligand Id: 2814] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL109581 |
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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 | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha | B | 5.75 | pKi | 1791 | nM | Ki | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR alpha | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta | B | 5.59 | pKi | 2587 | nM | Ki | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR beta | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
| ChEMBL | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma | B | 5.22 | pKi | 6094 | nM | Ki | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR gamma | B | 6.72 | pEC50 | 192 | nM | EC50 | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Inhibition of [3H]targretin binding to Retinoid X receptor RXR alpha | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - | Mol Endocrinol (2001) 15: 1360-9 [PMID:11463859] |
| ChEMBL | Transcriptional ativation of Retinoid X receptor RXR alpha | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702] | ||||||||
| ChEMBL | Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR beta | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| GtoPdb | - | - | 8 | pIC50 | - | - | - |
Mol Endocrinol (2001) 15: 1360-9 [PMID:11463859]; J Biol Chem (2002) 277: 12503-6 [PMID:11877384]; Nature (1996) 383: 450-3 [PMID:8837780] |
| ChEMBL | Transcriptional activation of Retinoid X receptor RXR beta | B | 7.89 | pEC50 | 13 | nM | EC50 | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443] | ||||||||
| ChEMBL | Inhibition of [3H]targretin binding to Retinoid X receptor RXR gamma | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
| ChEMBL | Transcriptional activation of Retinoid X receptor RXR gamma | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (1996) 39: 3229-3234 [PMID:8765503] |
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]
