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 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]