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Assay Detail

CHEMBL3268702

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

Binding
Inhibition of recombinant GGDPS (unknown origin) assessed as decrease in radiolabeld GGPP level using FPP and [14C]IPP as substrate treated with enzyme for 10 mins prior to substrate challenge for 30 mins by liquid scintillation counting analysis
6
Total Activities
6
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

Geranylgeranyl pyrophosphate synthase (CHEMBL4769)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Geranyl and neryl triazole bisphosphonates as inhibitors of geranylgeranyl diphosphate synthase.
Zhou X, Ferree SD, Wills VS, Born EJ, Tong H, Wiemer DF, Holstein SA.
Bioorg Med Chem (2014) 22 : 2791 -2798
PubMed 24726306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.49 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258994 DIGERANYL BISPHOSPHONATE 1 6.70
CHEMBL3262352 1 6.42
CHEMBL2315880 1 5.66
CHEMBL3262351 1 4.77
CHEMBL3262354 1 4.77
CHEMBL3262353 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258994 DIGERANYL BISPHOSPHONATE IC50 = 200.0 nM 6.70
CHEMBL3262352 IC50 = 380.0 nM 6.42
CHEMBL2315880 IC50 = 2200.0 nM 5.66
CHEMBL3262351 IC50 = 17000.0 nM 4.77
CHEMBL3262354 IC50 = 17000.0 nM 4.77
CHEMBL3262353 IC50 = 23000.0 nM 4.64