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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 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]