G15 [Ligand Id: 3320] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL583543
  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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  • GPER/G-protein coupled estrogen receptor 1 in Human [ChEMBL: CHEMBL5872] [GtoPdb: 221] [UniProtKB: Q99527]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Binding affinity to ERbeta receptor in COS7 cells by competitive binding assay B 5 pKi >10000 nM Ki Nat. Chem. Biol. (2009) 5: 421-427 [PMID:19430488]
GPER/G-protein coupled estrogen receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5872] [GtoPdb: 221] [UniProtKB: Q99527]
ChEMBL Binding affinity to GPR30 in human Hec50 cells by competitive binding assay B 7.7 pKi 20 nM Ki Nat. Chem. Biol. (2009) 5: 421-427 [PMID:19430488]
GtoPdb - - 6.7 pIC50 199 nM IC50 Nat Chem Biol (2009) 5: 421-7 [PMID:19430488]
ChEMBL Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of E2-mediated calcium mobilization F 6.72 pIC50 190 nM IC50 Nat. Chem. Biol. (2009) 5: 421-427 [PMID:19430488]
ChEMBL Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of G1-mediated calcium mobilization F 6.73 pIC50 185 nM IC50 Nat. Chem. Biol. (2009) 5: 421-427 [PMID:19430488]
ChEMBL Binding affinity to GPR30 B 7.7 pIC50 20 nM IC50 J. Med. Chem. (2010) 53: 1004-1014 [PMID:20041667]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]