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Assay Detail

CHEMBL2049637

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

Binding
Inhibition of human recombinant N-terminal-His6 tagged FPPS expressed in Escherichia coli BL21 using [3H]IPP and GPP as substrate incubated for 10 mins prior to substrate addition measured after 20 mins by liquid scintillation counting
1
Total Activities
1
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

Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.
Lin YS, Park J, De Schutter JW, Huang XF, Berghuis AM, Sebag M, Tsantrizos YS.
J Med Chem (2012) 55 : 3201 -3215
PubMed 22390415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.39 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID 4.0 1 8.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID IC50 = 4.1 nM 8.39