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ChEMBL ligand: CHEMBL258994 (Digeranyl Bisphosphonate) |
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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 [14C]IPP and GPP as substrate incubated for 10 mins prior to substrate addition measured after 10 mins by scintillation counting | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 3201-3215 [PMID:22390415] |
ChEMBL | Inhibition of human FPPS | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2013) 21: 2229-2240 [PMID:23477945] |
geranylgeranyl diphosphate synthase/Geranylgeranyl pyrophosphate synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4769] [GtoPdb: 643] [UniProtKB: O95749] | ||||||||
GtoPdb | Inhibition of human recombinant geranylgeranyl diphosphate synthase | - | 6 | pIC50 | - | - | - | J Med Chem (2008) 51: 5594-607 [PMID:18800762] |
ChEMBL | Inhibition of human recombinant geranylgeranyl diphosphate synthase | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2008) 51: 5594-5607 [PMID:18800762] |
ChEMBL | Inhibition of human recombinant geranylgeranyl diphosphate synthase | B | 6.01 | pIC50 | 980 | nM | IC50 | J Med Chem (2008) 51: 5594-5607 [PMID:18800762] |
ChEMBL | Inhibition of human N-terminal His6-tagged GGPPS Y246D mutant expressed in Escherichia coli BL21(DE3) using [14C]-IPP and FPP as substrates after 10 mins by scintillation counting | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2018) 61: 6904-6917 [PMID:30016091] |
ChEMBL | Inhibition of human N-terminal His6-tagged GGPPS expressed in Escherichia coli BL21(DE3) using [14C]-IPP and FPP as substrates after 10 mins by scintillation counting | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2018) 61: 6904-6917 [PMID:30016091] |
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 | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (2012) 55: 3201-3215 [PMID:22390415] |
ChEMBL | Inhibition of recombinant GGDPS (unknown origin) assessed as decrease in radiolabeld GGPP level using FPP and [14C]IPP as substrate treated with enzyme for 10 mins prior to substrate challenge for 30 mins by liquid scintillation counting analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2014) 22: 2791-2798 [PMID:24726306] |
ChEMBL | Inhibition of GST-tagged human recombinant GGDPS expressed in BL21 gold bacteria | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2008) 16: 390-399 [PMID:17905588] |
ChEMBL | Inhibition of human recombinant GGDPS expressed in BL21 gold bacteria | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2008) 16: 3652-3660 [PMID:18308574] |
GtoPdb | recombinant human protein expressed in BL21 gold bacteria, purified, in vitro assay | - | 6.7 | pIC50 | 200 | nM | IC50 | Biochem Biophys Res Commun (2007) 353: 921-5 [PMID:17208200] |
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]