ChEMBL ligand: CHEMBL924 (Anhydrous zoledronic acid, Zoledronate, Zoledronic acid anhydrous)
farnesyl diphosphate synthase/Farnesyl pyrophosphate synthase in Human [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324] farnesyl diphosphate synthase in Rat [GtoPdb: 644] [UniProtKB: P05369] There should be some charts here, you may need to enable JavaScript!
geranylgeranyl diphosphate synthase/Geranylgeranyl pyrophosphate synthase in Human [ChEMBL: CHEMBL4769] [GtoPdb: 643] [UniProtKB: O95749] 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 pyrophosphate synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1782] [GtoPdb: 644] [UniProtKB: P14324]
GtoPdb	Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins	-	7.07	pKi	85.9	nM	Ki	J Med Chem (2008) 51: 2187-95 [PMID:18327899]
GtoPdb	Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins	-	10.15	pKi	0.07	nM	Ki	J Med Chem (2008) 51: 2187-95 [PMID:18327899]
ChEMBL	Inhibition of human recombinant FPPS using IPP as substrate preincubated with enzyme for 15 mins followed by substrate addition and measured after 1 hr	B	6.26	pIC50	550	nM	IC50	Eur J Med Chem (2024) 276: 116679-116679 [PMID:39018923]
GtoPdb	Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins	-	6.32	pIC50	475.3	nM	IC50	J Med Chem (2008) 51: 2187-95 [PMID:18327899]
GtoPdb	Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins	-	8.39	pIC50	4.1	nM	IC50	J Med Chem (2008) 51: 2187-95 [PMID:18327899]
GtoPdb	Inhibition of human FPP synthase expressed in Escherichia coli BL21 (DE3)	-	8.39	pIC50	4.1	nM	IC50	J Med Chem (2008) 51: 6800-7 [PMID:18937434]
farnesyl diphosphate synthase in Rat [GtoPdb: 644] [UniProtKB: P05369]
GtoPdb	in vitro using kidney cell lines	-	6.3	pIC50	500	nM	IC50	Toxicol In Vitro (2008) 22: 899-909 [PMID:18325729]
geranylgeranyl diphosphate synthase/Geranylgeranyl pyrophosphate synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4769] [GtoPdb: 643] [UniProtKB: O95749]
ChEMBL	In Vitro hGGPPS Inhibition Assay: The assay was based on a literature procedure (Kavanagh, et al. J. Biol. Chem., 2006, 281, 22004-22012) with minor modifications. All assays were run in triplicate using recombinant human GGPPS (80 ng), FPP (10 μM), IPP (8.3 μM; 3H-IPP, 40 mCi/mmoL) in a final volume of 100 μL buffer containing 50 mM Tris pH 7.7, 2 mM MgCl2, 1 mM TCEP, 5 μg/mL BSA and 0.2% (w/v) Tween 20. The enzyme and test compound were pre-incubated in the assay buffer in a volume of 80 μL at 37° C. for 10 mins. Afterwards, the substrates (FPP, IPP) were added to start the reaction, which also bring the compound, substrate, and buffer contents to the desired final concentrations as indicated above. The assay mixture was then incubated at 37° C. for 15 mins (Note: the incubation time is based from the curve determined each time a new batch of enzyme is produced). Assays were terminated by the addition of 200 μL of HCl/MeOH (1:4) and incubated for 10 min at 37° C. The mixture was then extracted with 700 μL of petroleum ether, dried through a plug of anhydrous Mg2SO4 and 300 μL of the dried ligroin phase was combined with 8 mL of scintillation cocktail. Finally, the radioactivity was counted using a Beckman Coulter LS6500 liquid scintillation counter.	B	5.3	pIC50	>5000	nM	IC50	US-11279719-B2. Substituted bicyclic pyrimidine-based compounds and compositions and uses thereof (2022)

ChEMBL data shown on this page come from version 36:

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]