GSK4716 [Ligand Id: 2835] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL193836 (GSK4716)
  • Alpha trans-inducing protein (VP16) in Herpes simplex virus (type 1 / strain 17) [ChEMBL: CHEMBL4218] [UniProtKB: P06492]
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  • Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508]
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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 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]