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Assay Detail

CHEMBL681673

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

Binding
In vitro inhibition of geranylgeranyltransferase.
10
Total Activities
10
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

Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase.
Curtin ML, Florjancic AS, Cohen J, Gu WZ, Frost DJ, Muchmore SW, Sham HL.
Bioorg Med Chem Lett (2003) 13 : 1367 -1371
PubMed 12657284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.28 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27843 1 6.82
CHEMBL28970 1 6.75
CHEMBL431884 1 6.64
CHEMBL28588 1 6.51
CHEMBL282959 1 6.19
CHEMBL28770 1 6.00
CHEMBL284448 1 6.00
CHEMBL28707 1 5.92
CHEMBL28490 1 5.72
CHEMBL28659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27843 IC50 = 150.0 nM 6.82
CHEMBL28970 IC50 = 180.0 nM 6.75
CHEMBL431884 IC50 = 230.0 nM 6.64
CHEMBL28588 IC50 = 310.0 nM 6.51
CHEMBL282959 IC50 = 650.0 nM 6.19
CHEMBL28770 IC50 = 1000.0 nM 6.00
CHEMBL284448 IC50 = 1000.0 nM 6.00
CHEMBL28707 IC50 = 1200.0 nM 5.92
CHEMBL28490 IC50 = 1900.0 nM 5.72
CHEMBL28659 IC50 - nM -