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Assay Detail

CHEMBL2156000

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

Binding
Inhibition of recombinant human FPPS expressed in Escherichia coli by scintillation counting
5
Total Activities
5
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

Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.
Mucha A, Kafarski P, Berlicki Ł.
J Med Chem (2011) 54 : 5955 -5980
PubMed 21780776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.61 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID 4.0 1 8.52
CHEMBL923 RISEDRONIC ACID 4.0 1 8.00
CHEMBL53950 INCADRONIC ACID 2.0 1 7.52
CHEMBL870 ALENDRONIC ACID 4.0 1 7.30
CHEMBL834 PAMIDRONIC ACID 4.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID IC50 = 3.0 nM 8.52
CHEMBL923 RISEDRONIC ACID IC50 = 10.0 nM 8.00
CHEMBL53950 INCADRONIC ACID IC50 = 30.0 nM 7.52
CHEMBL870 ALENDRONIC ACID IC50 = 50.0 nM 7.30
CHEMBL834 PAMIDRONIC ACID IC50 = 200.0 nM 6.70