G-1 [Ligand Id: 1014] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
