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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL569766
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
There should be some charts here, you may need to enable JavaScript!
  • GPER/G-protein coupled estrogen receptor 1 in Human [ChEMBL: CHEMBL5872] [GtoPdb: 221] [UniProtKB: Q99527]
There should be some charts here, you may need to enable JavaScript!
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 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]