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ChEMBL ligand: CHEMBL569766 |
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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-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | Binding affinity to ERalpha receptor in COS7 cells by competitive binding assay | B | 5 | pKi | >10000 | nM | Ki | Nat Chem Biol (2009) 5: 421-427 [PMID:19430488] |
ChEMBL | Displacement of E2-Alexa633 from GFP-tagged ERalpha expressed in COS7 cells by FACS | B | 5 | pKi | >10000 | nM | Ki | Nat Chem Biol (2006) 2: 207-212 [PMID:16520733] |
GPER/G-protein coupled estrogen receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5872] [GtoPdb: 221] [UniProtKB: Q99527] | ||||||||
ChEMBL | Displacement of E2-Alexa633 from GFP-tagged GPR30 expressed in COS7 cells by FACS | B | 7.96 | pKi | 11 | nM | Ki | Nat Chem Biol (2006) 2: 207-212 [PMID:16520733] |
ChEMBL | Inhibition of estrogen binding to GPR30 (unknown origin) | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
GtoPdb | - | - | 8 | pKi | 10 | nM | Ki | Nat Chem Biol (2006) 2: 207-12 [PMID:16520733] |
ChEMBL | Binding affinity to GPR30 in human Hec50 cells by competitive binding assay | B | 8.15 | pKi | 7 | nM | Ki | Nat Chem Biol (2009) 5: 421-427 [PMID:19430488] |
ChEMBL | Binding affinity to GPR30 | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2010) 53: 1004-1014 [PMID:20041667] |
ChEMBL | Agonist activity at GPER (unknown origin) expressed in human HL60 cells assessed as increase in cAMP accumulation in presence of IBMX after 15 mins by HTRF assay | F | 5.84 | pEC50 | 1450 | nM | EC50 | ACS Med Chem Lett (2018) 9: 901-906 [PMID:30258538] |
ChEMBL | Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry | F | 8.7 | pEC50 | 2 | nM | EC50 | Nat Chem Biol (2006) 2: 207-212 [PMID:16520733] |
ChEMBL | Agonist activity at GPR30 (unknown origin) by calcium mobilization assay | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
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]