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Assay Detail

CHEMBL4337920

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

Binding
Inhibition of N-terminal His-tagged human FPPS (1 to 353 residues) expressed in Escherichia coli BL21 (DE3) pre-incubated for 10 mins before addition of GPP and [14C]-IPP by scintillation counting method
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

Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).
Feng Y, Park J, Li SG, Boutin R, Viereck P, Schilling MA, Berghuis AM, Tsantrizos YS.
J Med Chem (2019) 62 : 9691 -9702
PubMed 31577901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.70 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID 4.0 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID IC50 = 2.0 nM 8.70