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ChEMBL ligand: CHEMBL583543 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
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]