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Assay Detail

CHEMBL680439

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

Binding
In vitro inhibitory activity against farnesyltransferase (FTase)
22
Total Activities
19
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

Protein farnesyltransferase (CHEMBL2095178)
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 22 8.28 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282959 1 9.43
CHEMBL27843 1 9.41
CHEMBL431884 1 9.35
CHEMBL289228 TIPIFARNIB 3.0 1 9.24
CHEMBL28707 1 9.01
CHEMBL29982 1 9.00
CHEMBL28252 2 8.82
CHEMBL29645 2 8.82
CHEMBL28770 1 8.82
CHEMBL29064 2 8.72
CHEMBL28970 1 8.72
CHEMBL298734 LONAFARNIB 4.0 1 8.11
CHEMBL284448 1 8.00
CHEMBL28659 1 7.96
CHEMBL28588 1 7.85
CHEMBL28490 1 7.75
CHEMBL28937 1 7.19
CHEMBL282368 1 7.08
CHEMBL27750 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282959 IC50 = 0.37 nM 9.43
CHEMBL27843 IC50 = 0.39 nM 9.41
CHEMBL431884 IC50 = 0.45 nM 9.35
CHEMBL289228 TIPIFARNIB IC50 = 0.57 nM 9.24
CHEMBL28707 IC50 = 0.97 nM 9.01
CHEMBL29982 IC50 = 1.0 nM 9.00
CHEMBL28252 IC50 = 1.5 nM 8.82
CHEMBL29645 IC50 = 1.5 nM 8.82
CHEMBL28770 IC50 = 1.5 nM 8.82
CHEMBL29064 IC50 = 1.9 nM 8.72
CHEMBL28970 IC50 = 1.9 nM 8.72
CHEMBL298734 LONAFARNIB IC50 = 7.8 nM 8.11
CHEMBL284448 IC50 = 10.0 nM 8.00
CHEMBL29645 IC50 = 11.0 nM 7.96
CHEMBL28659 IC50 = 11.0 nM 7.96
CHEMBL28588 IC50 = 14.0 nM 7.85
CHEMBL28490 IC50 = 18.0 nM 7.75
CHEMBL29064 IC50 = 31.0 nM 7.51
CHEMBL28252 IC50 = 38.0 nM 7.42
CHEMBL28937 IC50 = 65.0 nM 7.19
CHEMBL282368 IC50 = 84.0 nM 7.08
CHEMBL27750 IC50 = 1000.0 nM 6.00