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Assay Detail

CHEMBL682065

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

Binding
Inhibition of Farnesyltransferase
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors.
Wang L, Wang GT, Wang X, Tong Y, Sullivan G, Park D, Leonard NM, Li Q, Cohen J, Gu WZ, Zhang H, Bauch JL, Jakob CG, Hutchins CW, Stoll VS, Marsh K, Rosenberg SH, Sham HL, Lin NH.
J Med Chem (2004) 47 : 612 -626
PubMed 14736242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.16 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41748 1 9.52
CHEMBL43631 1 9.40
CHEMBL351706 BMS-214662 1.0 1 9.15
CHEMBL289228 TIPIFARNIB 3.0 1 9.05
CHEMBL298734 LONAFARNIB 4.0 1 8.70
CHEMBL279433 L-778123 FREE BASE 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41748 IC50 = 0.3 nM 9.52
CHEMBL43631 IC50 = 0.4 nM 9.40
CHEMBL351706 BMS-214662 IC50 = 0.7 nM 9.15
CHEMBL289228 TIPIFARNIB IC50 = 0.9 nM 9.05
CHEMBL298734 LONAFARNIB IC50 = 2.0 nM 8.70
CHEMBL279433 L-778123 FREE BASE IC50 = 2.0 nM -