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 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]