22R-hydroxycholesterol [Ligand Id: 2742] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL422904 (22(R)-Hydroxycholesterol) |
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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 | Effective concentration for cofactor association with recombinant liver X receptor-alpha | B | 4.82 | pEC50 | 15000 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2824-2828 [PMID:15911262] |
| ChEMBL | Agonist activity at human recombinant LXRalpha expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRalpha ligand binding domain by HTRF assay | B | 4.82 | pEC50 | >15000 | nM | EC50 | J Nat Prod (2005) 68: 1247-1252 [PMID:16124770] |
| ChEMBL | Activation of GAL4 fused human LXR alpha expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 5.17 | pEC50 | 6710 | nM | EC50 | J Med Chem (2017) 60: 6548-6562 [PMID:28741954] |
| GtoPdb | - | - | 5.3 | pEC50 | - | - | - | Nature (1996) 383: 728-31 [PMID:8878485] |
| ChEMBL | Agonist activity at human LXRalpha-LBD assessed as recruitment of co-activator peptide after 2 hrs by TR-FRET assay | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4185-4190 [PMID:23769638] |
| ChEMBL | Concentration required for half maximal activity was calculated in human nuclear oxysterol receptor liver X receptor-alpha in LiSA. | B | 6.49 | pEC50 | 325 | nM | EC50 | J Med Chem (2001) 44: 886-897 [PMID:11300870] |
| Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
| ChEMBL | Effective concentration for cofactor association with recombinant liver X receptor-beta | B | 4.82 | pEC50 | 15000 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2824-2828 [PMID:15911262] |
| ChEMBL | Agonist activity at human recombinant LXRbeta expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRbeta ligand binding domain by HTRF assay | B | 4.82 | pEC50 | >15000 | nM | EC50 | J Nat Prod (2005) 68: 1247-1252 [PMID:16124770] |
| ChEMBL | Activation of GAL4 fused human LXR beta expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 5.32 | pEC50 | 4750 | nM | EC50 | J Med Chem (2017) 60: 6548-6562 [PMID:28741954] |
| GtoPdb | - | - | 5.52 | pEC50 | - | - | - | Nature (1996) 383: 728-31 [PMID:8878485] |
| RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449] | ||||||||
| ChEMBL | Agonist activity at human His6-tagged ROR gamma ligand binding domain (residues 262 to 507) expressed in Escherichia coli BL21 (DE3) cells assessed as increase in recruitment of coactivator peptide by AlphaScreen biochemical assay | B | 7.7 | pEC50 | 20 | nM | EC50 | Medchemcomm (2013) 4: 764-776 |
| ChEMBL | Displacement of [3H]25-hydroxycholesterol from human RORc-LBD expressed in bacterial expression system after 3 hrs by scintillation counting analysis | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5769-5776 [PMID:25453817] |
| ChEMBL | Agonist activity at 6xHis tagged human RORgammat LBD (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) assessed as biotinylated SRC1-2 peptide coactivator recruitment by AlphaScreen assay | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2018) 61: 5794-5804 [PMID:29412659] |
| Farnesoid X receptor in Human [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| GtoPdb | - | - | 5.5 | pEC50 | - | - | - | J Pharmacol Exp Ther (2006) 317: 317-25 [PMID:16371446] |
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]
