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Assay Detail

CHEMBL683492

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

Binding
Inhibition of Geranylgeranyl transferase type I, an enzyme that recognizes CaaX sequences containing leucine as the terminal residue.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Geranylgeranyl transferase type I (CHEMBL2096987)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

DIARYLETHER INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
Dinsmore* CJ, Williams TM, Hamilton K, O'Neill TJ, Rands E, Koblan KS, Kohl NE, Gibbs JB, Graham SL, Hartman GD, Oliff AI
Bioorg Med Chem Lett (1997) 7 : 1345 -1348
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.39 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26149 1 5.64
CHEMBL26255 1 5.30
CHEMBL25734 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26149 IC50 = 2300.0 nM 5.64
CHEMBL26255 IC50 = 5000.0 nM 5.30
CHEMBL25734 IC50 = 5800.0 nM 5.24