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Assay Detail

CHEMBL677586

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

Binding
Inhibitory activity against the human recombinant FPPSase (Farnesyl diphosphate) enzyme
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.
Szabo CM, Matsumura Y, Fukura S, Martin MB, Sanders JM, Sengupta S, Cieslak JA, Loftus TC, Lea CR, Lee HJ, Koohang A, Coates RM, Sagami H, Oldfield E.
J Med Chem (2002) 45 : 2185 -2196
PubMed 12014956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.05 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL923 RISEDRONIC ACID 4.0 1 8.00
CHEMBL997 IBANDRONIC ACID 4.0 1 7.70
CHEMBL870 ALENDRONIC ACID 4.0 1 7.30
CHEMBL834 PAMIDRONIC ACID 4.0 1 6.70
CHEMBL293522 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL923 RISEDRONIC ACID IC50 = 10.0 nM 8.00
CHEMBL997 IBANDRONIC ACID IC50 = 20.0 nM 7.70
CHEMBL870 ALENDRONIC ACID IC50 = 50.0 nM 7.30
CHEMBL834 PAMIDRONIC ACID IC50 = 200.0 nM 6.70
CHEMBL293522 IC50 = 2930.0 nM 5.53