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Assay Detail

CHEMBL1036745

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

Binding
Inhibition of human FPP synthase expressed in Escherichia coli BL21 (DE3)
7
Total Activities
7
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

Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism.
Simoni D, Gebbia N, Invidiata FP, Eleopra M, Marchetti P, Rondanin R, Baruchello R, Provera S, Marchioro C, Tolomeo M, Marinelli L, Limongelli V, Novellino E, Kwaasi A, Dunford J, Buccheri S, Caccamo N, Dieli F.
J Med Chem (2008) 51 : 6800 -6807
PubMed 18937434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.11 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID 4.0 1 8.39
CHEMBL446734 1 8.04
CHEMBL457423 1 7.79
CHEMBL504429 1 7.55
CHEMBL457424 1 6.41
CHEMBL452354 1 6.05
CHEMBL457069 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303669 ZOLEDRONIC ACID IC50 = 4.1 nM 8.39
CHEMBL446734 IC50 = 9.03 nM 8.04
CHEMBL457423 IC50 = 16.1 nM 7.79
CHEMBL504429 IC50 = 28.1 nM 7.55
CHEMBL457424 IC50 = 388.2 nM 6.41
CHEMBL452354 IC50 = 883.1 nM 6.05
CHEMBL457069 IC50 = 3069.0 nM 5.51