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Assay Detail

CHEMBL682095

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

Binding
Inhibition of Farnesyltransferase
4
Total Activities
4
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

Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.
Njoroge FG, Vibulbhan B, Pinto P, Bishop WR, Bryant MS, Nomeir AA, Lin C, Liu M, Doll RJ, Girijavallabhan V, Ganguly AK.
J Med Chem (1998) 41 : 1561 -1567
PubMed 9572881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.34 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41473 1 7.52
CHEMBL39153 1 7.40
CHEMBL416231 1 7.40
CHEMBL41934 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41473 IC50 = 30.0 nM 7.52
CHEMBL39153 IC50 = 40.0 nM 7.40
CHEMBL416231 IC50 = 40.0 nM 7.40
CHEMBL41934 IC50 = 90.0 nM 7.05