BMS-852927 [Ligand Id: 14079] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3945199 (Bms-852927, EXEL-04541041, XL-041, XL-652) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] | ||||||||
| ChEMBL | Antagonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs in presence of LXR pan agonist 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile by luciferase reporter gene assay | B | 7.16 | pIC50 | 69 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
| ChEMBL | Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay | B | 7.62 | pEC50 | 24 | nM | EC50 | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| ChEMBL | Agonist activity at LXR-beta in human whole blood assessed as ABCG1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis | B | 8 | pEC50 | 10 | nM | EC50 | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| ChEMBL | Agonist activity at LXR-beta in human whole blood assessed as ABCA1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis | B | 8.05 | pEC50 | 9 | nM | EC50 | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| GtoPdb | - | - | 8.05 | pEC50 | 9 | nM | EC50 | Cell Metab (2016) 24: 223-33 [PMID:27508871] |
| ChEMBL | Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay | B | 9.22 | pEC50 | 0.6 | nM | EC50 | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Agonist activity at human PXR expressed in human HepG2 cells assessed as induction of CYP3A4 measured after 24 hrs by AlamarBlue dye-based luciferase reporter gene assay | B | 6 | pEC50 | 1000 | nM | EC50 | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| Retinoid X receptor-α/Liver X receptor-α/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430879] [GtoPdb: 610, 602] [UniProtKB: P19793, Q13133] | ||||||||
| ChEMBL | Displacement of [3H]-24,25-epoxycholesterol from human LXRalpha/RXRalpha expressed in baculovirus infected Sf9 cells by scintillation proximity analysis | B | 7.72 | pKi | 19 | nM | Ki | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| Retinoid X receptor-α/Liver X receptor-β/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430878] [GtoPdb: 610, 601] [UniProtKB: P19793, P55055] | ||||||||
| ChEMBL | Displacement of [3H]-24,25-epoxycholesterol from human LXRbeta/RXRalpha expressed in baculovirus infected Sf9 cells by scintillation proximity analysis | B | 7.92 | pKi | 12 | nM | Ki | ACS Med Chem Lett (2016) 7: 1207-1212 [PMID:27994765] |
| GtoPdb | - | - | 8.05 | pEC50 | 9 | nM | EC50 | Cell Metab (2016) 24: 223-33 [PMID:27508871] |
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]
