GSK4716 [Ligand Id: 2835] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL193836 (GSK4716) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Alpha trans-inducing protein (VP16) in Herpes simplex virus (type 1 / strain 17) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4218] [UniProtKB: P06492] | ||||||||
| ChEMBL | Agonist activity at Herpes simplex virus Gal4 fused VP16-LBD expressed in HEK293T cells after 20 hrs by UAS-luciferase reporter gene assay | B | 6.56 | pEC50 | 272.6 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1313-1319 [PMID:29548571] |
| Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508] | ||||||||
| ChEMBL | Binding affinity to ERRgamma (unknown origin) at 20 degC by isothermal titration calorimetry | B | 5.3 | pKd | 5000 | nM | Kd | Bioorg Med Chem (2015) 23: 3751-3760 [PMID:25910584] |
| ChEMBL | Inhibition of [3H]4-OHT binding to Estrogen-Related Receptor gamma | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2005) 48: 3107-3109 [PMID:15857113] |
| GtoPdb | - | - | 5.7 | pIC50 | - | - | - | J Med Chem (2005) 48: 3107-9 [PMID:15857113] |
| ChEMBL | Agonist activity at Gal4 fused ERRgamma-LBD (unknown origin) expressed in HEK293T cells after 20 hrs by UAS-luciferase reporter gene assay | B | 5.72 | pEC50 | 1899 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1313-1319 [PMID:29548571] |
| ChEMBL | Estrogen-Related Receptor gamma activity in FRET assay | F | 5.89 | pEC50 | 1300 | nM | EC50 | J Med Chem (2005) 48: 3107-3109 [PMID:15857113] |
| ChEMBL | Agonist activity at human N-terminal alphaHis-SUMO-tagged ERRgamma-LBD (229 to 458 residues) expressed in Escherichia coli BL21 gold (DE3) cells assessed as decrease in RIP140 peptide recruitment after 2 hrs by TR-FRET assay | B | 6.22 | pEC50 | 600 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1313-1319 [PMID:29548571] |
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]
