toremifene [Ligand Id: 4325] 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: CHEMBL1655 (Acapodene, Chlortamoxifen, Farestone, GTX-006, J33.157K, Toremifene, Toremiphene)
  • Envelope glycoprotein in Zaire ebolavirus (strain Mayinga-76) (ZEBOV) (Zaire Ebola virus) [ChEMBL: CHEMBL4105829] [UniProtKB: Q05320]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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
Envelope glycoprotein in Zaire ebolavirus (strain Mayinga-76) (ZEBOV) (Zaire Ebola virus) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105829] [UniProtKB: Q05320]
ChEMBL Binding affinity to Ebola virus Zaire Mayinga-76 recombinant GP protein by SYPRO orange dye-based fluorescence assay B 4.8 pKd 16000 nM Kd J Med Chem (2018) 61: 724-733 [PMID:29272110]
ChEMBL Binding affinity to EBOV Mayinga, Zaire, 1976 envelope glycoprotein extracellular domain T42A mutant tagged with 6xHis/foldon trimerization sequence from the bacteriophage T4 fibritin at C terminal expressed in HEK293T cells at pH 5.2 by SYPRO orange dye-based fluorescence assay B 4.8 pKd 16000 nM Kd J Med Chem (2018) 61: 4938-4945 [PMID:29741894]
ChEMBL Inhibition of HIV/EBOV GP Y517S mutant infected in 293T cells assessed as reduction in virus entry B 7.2 pEC50 62.8 nM EC50 J Med Chem (2020) 63: 7211-7225 [PMID:32490678]
ChEMBL Inhibition of HIV/EBOV GP T519V mutant infected in 293T cells assessed as reduction in virus entry B 7.2 pEC50 62.8 nM EC50 J Med Chem (2020) 63: 7211-7225 [PMID:32490678]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting B 5.38 pKi 4125 nM Ki J Med Chem (2012) 55: 5704-5719 [PMID:22537153]

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]