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ChEMBL ligand: CHEMBL2048241 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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farnesyl diphosphate synthase/Farnesyl diphosphate synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324] | ||||||||
ChEMBL | Inhibition of human recombinant N-terminal-His6 tagged FPPS expressed in Escherichia coli BL21 using [3H]IPP and GPP as substrate measured after 20 mins by liquid scintillation counting | B | 5.86 | pIC50 | 1390 | nM | IC50 | J Med Chem (2012) 55: 3201-3215 [PMID:22390415] |
ChEMBL | Inhibition of human recombinant N-terminal-His6 tagged FPPS expressed in Escherichia coli BL21 using [14C]IPP and GPP as substrate incubated for 10 mins prior to substrate addition measured after 10 mins by scintillation counting | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2012) 55: 3201-3215 [PMID:22390415] |
ChEMBL | Inhibition of human His6-tagged recombinant FPPS expressed in Escherichia coli BL21(DE3) using GPP and [3H]IPP as substrate incubated for 5 mins prior to substrate addition measured after 20 mins by liquid scintillation counting | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem (2012) 20: 5583-5591 [PMID:22884353] |
geranylgeranyl diphosphate synthase/Geranylgeranyl pyrophosphate synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4769] [GtoPdb: 643] [UniProtKB: O95749] | ||||||||
ChEMBL | Inhibition of human recombinant N-terminal His6 tagged GGPPS expressed in Escherichia coli BL21 using FPP and [14C]IPP as substrate incubated for 10 mins prior to substrate addition by scintillation counting | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 3201-3215 [PMID:22390415] |
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]