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Assay Detail

CHEMBL4267725

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

Binding
Inhibition of recombinant human C-terminal His6-tagged FPPS expressed in Escherichia coli BL21 using DMAPP and IPP as substrates pretreated for 15 mins followed by substrates addition and measured after 1 hr by colorimetric method
4
Total Activities
4
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

Novel bisphosphonates with antiresorptive effect in bone mineralization and osteoclastogenesis.
Savino S, Toscano A, Purgatorio R, Profilo E, Laghezza A, Tortorella P, Angelelli M, Cellamare S, Scala R, Tricarico D, Marobbio CMT, Perna F, Vitale P, Agamennone M, Dimiccoli V, Tolomeo A, Scilimati A.
Eur J Med Chem (2018) 158 : 184 -200
PubMed 30216851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.32 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID 4.0 1 7.22
CHEMBL923 RISEDRONIC ACID 4.0 1 7.16
CHEMBL4283512 1 6.51
CHEMBL4279995 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID IC50 = 60.0 nM 7.22
CHEMBL923 RISEDRONIC ACID IC50 = 70.0 nM 7.16
CHEMBL4283512 IC50 = 310.0 nM 6.51
CHEMBL4279995 IC50 = 41000.0 nM 4.39