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Assay Detail

CHEMBL902037

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

Binding
Inhibition of human cloned FPPS expressed in Escherichia col BL2 (DE3)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
Marma MS, Xia Z, Stewart C, Coxon F, Dunford JE, Baron R, Kashemirov BA, Ebetino FH, Triffitt JT, Russell RG, McKenna CE.
J Med Chem (2007) 50 : 5967 -5975
PubMed 17975902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.19 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437758 1 7.79
CHEMBL98110 1 7.47
CHEMBL394758 1 7.02
CHEMBL394759 1 6.47
CHEMBL240775 1 -
CHEMBL240772 1 -
CHEMBL240771 1 -
CHEMBL397829 1 -
CHEMBL240776 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437758 IC50 = 16.4 nM 7.79
CHEMBL98110 IC50 = 34.2 nM 7.47
CHEMBL394758 IC50 = 94.6 nM 7.02
CHEMBL394759 IC50 = 340.4 nM 6.47
CHEMBL240775 IC50 > 60000.0 nM -
CHEMBL240772 IC50 > 600000.0 nM -
CHEMBL240771 IC50 > 600000.0 nM -
CHEMBL397829 IC50 = 253500.0 nM -
CHEMBL240776 IC50 - -