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ChEMBL ligand: CHEMBL494897 (BPH-715) |
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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 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 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]