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Assay Detail

CHEMBL5615210

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant FPPS using IPP as substrate preincubated with enzyme for 15 mins followed by substrate addition and measured after 1 hr
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Farnesyl pyrophosphate synthase (CHEMBL1782)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Farnesyl pyrophosphate synthase inhibitors with antiosteoporosis efficacy in ovariectomized rats: A mixed binding approach beyond bisphosphonates.
El-Sayed NF, El-Hussieny M, Mansour ST, Fouad MA, Saad MA, Ewies EF.
Eur J Med Chem (2024) 276 : 116679 -116679
PubMed 39018923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.40 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL924 ZOLEDRONIC ACID ANHYDROUS 4.0 1 6.26
CHEMBL5619915 1 5.96
CHEMBL5618314 1 5.91
CHEMBL5618430 1 5.61
CHEMBL5618141 1 5.49
CHEMBL5619264 1 5.47
CHEMBL5618666 1 5.26
CHEMBL5619062 1 5.22
CHEMBL5619109 1 4.90
CHEMBL5619920 1 4.67
CHEMBL5619599 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL924 ZOLEDRONIC ACID ANHYDROUS IC50 = 550.0 nM 6.26
CHEMBL5619915 IC50 = 1108.0 nM 5.96
CHEMBL5618314 IC50 = 1240.0 nM 5.91
CHEMBL5618430 IC50 = 2471.0 nM 5.61
CHEMBL5618141 IC50 = 3216.0 nM 5.49
CHEMBL5619264 IC50 = 3374.0 nM 5.47
CHEMBL5618666 IC50 = 5543.0 nM 5.26
CHEMBL5619062 IC50 = 5980.0 nM 5.22
CHEMBL5619109 IC50 = 12560.0 nM 4.90
CHEMBL5619920 IC50 = 21430.0 nM 4.67
CHEMBL5619599 IC50 = 22660.0 nM 4.64