22R-hydroxycholesterol [Ligand Id: 2742] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL422904 (22(R)-Hydroxycholesterol) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
