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 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]
