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Assay Detail

CHEMBL828106

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

Binding
Inhibition of [3H]FPP incorporation into recombinant Ras CVIM by human Farnesyltransferase
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Lin NH, Wang L, Wang X, Wang GT, Cohen J, Gu WZ, Zhang H, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2004) 14 : 5057 -5062
PubMed 15380198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 9.49 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361246 1 11.00
CHEMBL426063 1 10.52
CHEMBL364792 1 10.00
CHEMBL184707 1 9.57
CHEMBL435285 1 9.51
CHEMBL184330 1 9.44
CHEMBL186906 1 9.43
CHEMBL181748 1 9.43
CHEMBL22702 1 9.43
CHEMBL187175 1 9.34
CHEMBL364165 1 9.22
CHEMBL362881 1 9.21
CHEMBL24043 1 9.14
CHEMBL184568 1 8.92
CHEMBL187375 1 8.92
CHEMBL187809 1 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361246 IC50 = 0.01 nM 11.00
CHEMBL426063 IC50 = 0.03 nM 10.52
CHEMBL364792 IC50 = 0.1 nM 10.00
CHEMBL184707 IC50 = 0.27 nM 9.57
CHEMBL435285 IC50 = 0.31 nM 9.51
CHEMBL184330 IC50 = 0.36 nM 9.44
CHEMBL186906 IC50 = 0.37 nM 9.43
CHEMBL181748 IC50 = 0.37 nM 9.43
CHEMBL22702 IC50 = 0.37 nM 9.43
CHEMBL187175 IC50 = 0.46 nM 9.34
CHEMBL364165 IC50 = 0.6 nM 9.22
CHEMBL362881 IC50 = 0.62 nM 9.21
CHEMBL24043 IC50 = 0.73 nM 9.14
CHEMBL184568 IC50 = 1.2 nM 8.92
CHEMBL187375 IC50 = 1.2 nM 8.92
CHEMBL187809 IC50 = 2.1 nM 8.68