Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL656841

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

Functional
In vitro inhibition of Ras processing in COS cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type COS
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
Wolin R, Connolly M, Kelly J, Weinstein J, Rosenblum S, Afonso A, James L, Kirschmeier P, Bishop WR.
Bioorg Med Chem Lett (1998) 8 : 2521 -2526
PubMed 9873573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.33 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289404 1 6.00
CHEMBL81889 1 5.77
CHEMBL311310 1 5.43
CHEMBL313193 1 5.42
CHEMBL315067 1 5.38
CHEMBL315599 1 5.30
CHEMBL423677 1 5.00
CHEMBL309483 1 5.00
CHEMBL84036 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289404 IC50 = 1000.0 nM 6.00
CHEMBL81889 IC50 = 1700.0 nM 5.77
CHEMBL311310 IC50 = 3700.0 nM 5.43
CHEMBL313193 IC50 = 3800.0 nM 5.42
CHEMBL315067 IC50 = 4200.0 nM 5.38
CHEMBL315599 IC50 = 5000.0 nM 5.30
CHEMBL423677 IC50 = 10000.0 nM 5.00
CHEMBL309483 IC50 = 10000.0 nM 5.00
CHEMBL84036 IC50 = 20000.0 nM 4.70