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Assay Detail

CHEMBL1109110

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

Binding
Inhibition of human FPPS after 10 mins using [14C]IPP as substrate by liquid scintillation counting
7
Total Activities
3
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

Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
McKenna CE, Kashemirov BA, Błazewska KM, Mallard-Favier I, Stewart CA, Rojas J, Lundy MW, Ebetino FH, Baron RA, Dunford JE, Kirsten ML, Seabra MC, Bala JL, Marma MS, Rogers MJ, Coxon FP.
J Med Chem (2010) 53 : 3454 -3464
PubMed 20394422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319144 MINODRONIC ACID 4.0 1 8.52
CHEMBL1099309 (2-HYDROXY-3-IMIDAZO[1,2-A]PYRIDIN-3-YL-2-PHOSPHONOPROPIONIC ACID (ENANTIONMERS) 3 -
CHEMBL397829 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319144 MINODRONIC ACID IC50 = 3.0 nM 8.52
CHEMBL1099309 (2-HYDROXY-3-IMIDAZO[1,2-A]PYRIDIN-3-YL-2-PHOSPHONOPROPIONIC ACID (ENANTIONMERS) IC50 > 10000.0 nM -
CHEMBL397829 IC50 > 1000000.0 nM -
CHEMBL397829 IC50 - -
CHEMBL397829 IC50 - -
CHEMBL1099309 (2-HYDROXY-3-IMIDAZO[1,2-A]PYRIDIN-3-YL-2-PHOSPHONOPROPIONIC ACID (ENANTIONMERS) IC50 - -
CHEMBL1099309 (2-HYDROXY-3-IMIDAZO[1,2-A]PYRIDIN-3-YL-2-PHOSPHONOPROPIONIC ACID (ENANTIONMERS) IC50 - -