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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 |
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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 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]