XCT790 [Ligand Id: 2832] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL189753 (XCT790)
  • Estrogen-related receptor-α/Estrogen-related receptor alpha in Human [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Estrogen-related receptor-α/Estrogen-related receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474]
ChEMBL Inhibition of estrogen-related receptor alpha Gal4 activity B 6.43 pIC50 370 nM IC50 J Med Chem (2004) 47: 5593-5596 [PMID:15509154]
ChEMBL Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay F 6.43 pIC50 370 nM IC50 J Med Chem (2011) 54: 788-808 [PMID:21218783]
ChEMBL Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay B 6.43 pIC50 370 nM IC50 J Med Chem (2013) 56: 4631-4640 [PMID:23656512]
ChEMBL Inverse agonist activity at CMX-gal4-fused ERRgamma (unknown origin) transfected in (African Green monkey CV1 cells incubated for 20 hrs by luciferase reporter gene assay B 6.43 pIC50 370 nM IC50 ACS Med Chem Lett (2019) 10: 767-772 [PMID:31097997]
GtoPdb - - 6.5 pIC50 - - IC50 Proc Natl Acad Sci USA (2004) 101: 8912-7 [PMID:15184675]
ChEMBL Inverse agonist activity at GAL4-DNA binding domain-fused human ERRalpha ligand binding domain expressed in HEK293 cells assessed as inhibition of transcriptional activity after 48 hrs by luciferase reporter gene assay B 6.57 pIC50 270 nM IC50 Eur J Med Chem (2017) 136: 457-467 [PMID:28525844]
ChEMBL Binding affinity to GST-tagged ERRalpha-LBD (unknown origin) using fluorescein-conjugated coactivator PGC-1alpha incubated for 1 hr by TR-FRET assay B 7.21 pIC50 61.33 nM IC50 ACS Med Chem Lett (2019) 10: 767-772 [PMID:31097997]

ChEMBL data shown on this page come from version 32:

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]