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Assay Detail

CHEMBL681811

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

Binding
Inhibition of [3H]FPP incorporation into biotinylated laminB peptide by farnesyl transferase
12
Total Activities
11
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

5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors.
Angibaud P, Bourdrez X, Devine A, End DW, Freyne E, Ligny Y, Muller P, Mannens G, Pilatte I, Poncelet V, Skrzat S, Smets G, Van Dun J, Van Remoortere P, Venet M, Wouters W.
Bioorg Med Chem Lett (2003) 13 : 1543 -1547
PubMed 12699751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.61 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39324 2 9.30
CHEMBL289228 TIPIFARNIB 3.0 1 9.10
CHEMBL289529 1 9.00
CHEMBL38080 1 8.80
CHEMBL290745 1 8.77
CHEMBL288853 1 8.46
CHEMBL288693 1 8.40
CHEMBL290833 1 8.22
CHEMBL39274 1 8.22
CHEMBL40088 1 8.19
CHEMBL289417 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39324 IC50 = 0.5 nM 9.30
CHEMBL39324 IC50 = 0.5 nM 9.30
CHEMBL289228 TIPIFARNIB IC50 = 0.8 nM 9.10
CHEMBL289529 IC50 = 1.0 nM 9.00
CHEMBL38080 IC50 = 1.6 nM 8.80
CHEMBL290745 IC50 = 1.7 nM 8.77
CHEMBL288853 IC50 = 3.5 nM 8.46
CHEMBL288693 IC50 = 4.0 nM 8.40
CHEMBL290833 IC50 = 6.0 nM 8.22
CHEMBL39274 IC50 = 6.0 nM 8.22
CHEMBL40088 IC50 = 6.5 nM 8.19
CHEMBL289417 IC50 = 29.0 nM 7.54