BPH-715 [Ligand Id: 3196] 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: CHEMBL494897 (BPH-715)
  • farnesyl diphosphate synthase/Farnesyl diphosphate synthase in Human [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324]
There should be some charts here, you may need to enable JavaScript!
  • geranylgeranyl diphosphate synthase/Geranylgeranyl pyrophosphate synthetase in Human [ChEMBL: CHEMBL4769] [GtoPdb: 643] [UniProtKB: O95749]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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
farnesyl diphosphate synthase/Farnesyl diphosphate synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324]
ChEMBL Inhibition of human FPPS using FPP and [3H]-IPP as substrate incubated for 30 mins prior to substrate addition measured after 20 mins by scintillation counting B 7 pIC50 100 nM IC50 J Med Chem (2012) 55: 3201-3215 [PMID:22390415]
ChEMBL Inhibition of human FPPS using GPP and [3H]IPP as substrate by scintillation counting B 7 pIC50 100 nM IC50 Bioorg Med Chem (2012) 20: 5583-5591 [PMID:22884353]
ChEMBL Inhibition of human FPPS using IPP and GPP B 7 pIC50 100 nM IC50 J Med Chem (2019) 62: 2564-2581 [PMID:30730737]
geranylgeranyl diphosphate synthase/Geranylgeranyl pyrophosphate synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4769] [GtoPdb: 643] [UniProtKB: O95749]
ChEMBL Inhibition of human GGPPS B 5.16 pKi 6900 nM Ki Antimicrob Agents Chemother (2010) 54: 2987-2993 [PMID:20457823]
GtoPdb Inhibition of human recombinant geranylgeranyl diphosphate synthase - 6.55 pIC50 280 nM IC50 J Med Chem (2008) 51: 5594-607 [PMID:18800762]
ChEMBL Inhibition of human recombinant geranylgeranyl diphosphate synthase B 6.55 pIC50 280 nM IC50 J Med Chem (2008) 51: 5594-5607 [PMID:18800762]
ChEMBL Inhibition of human recombinant GGPPS using [14C]-IPP as substrate incubated for 15 mins prior to substrate addition measured after 20 mins by scintillation counting B 6.55 pIC50 280 nM IC50 J Med Chem (2012) 55: 3201-3215 [PMID:22390415]
ChEMBL Inhibition of human recombinant GGPS using [14C]-IPP as substrate incubated for 15 mins prior to substrate addition measured after 20 mins by scintillation counting B 6.55 pIC50 280 nM IC50 Bioorg Med Chem (2012) 20: 5583-5591 [PMID:22884353]
ChEMBL Inhibition of human GGPPS B 6.55 pIC50 280 nM IC50 J Med Chem (2019) 62: 2564-2581 [PMID:30730737]
ChEMBL Inhibition of human recombinant geranylgeranyl diphosphate synthase B 6.6 pIC50 251.19 nM IC50 J Med Chem (2008) 51: 5594-5607 [PMID:18800762]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL Antimalarial activity against Plasmodium berghei NK65 infected in human HepG2 cells after 48 hrs by RT-PCR F 5 pIC50 10000 nM IC50 Antimicrob Agents Chemother (2010) 54: 2987-2993 [PMID:20457823]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as suppression of parasitemia by microscopic analysis F 6.17 pIC50 670 nM IC50 Antimicrob Agents Chemother (2010) 54: 2987-2993 [PMID:20457823]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2mef assessed as suppression of parasitemia by microscopic analysis F 6.23 pIC50 590 nM IC50 Antimicrob Agents Chemother (2010) 54: 2987-2993 [PMID:20457823]

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]