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Assay Detail

CHEMBL681807

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
11
Total Activities
7
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

Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Angibaud P, Bourdrez X, End DW, Freyne E, Janicot M, Lezouret P, Ligny Y, Mannens G, Damsch S, Mevellec L, Meyer C, Muller P, Pilatte I, Poncelet V, Roux B, Smets G, Van Dun J, Van Remoortere P, Venet M, Wouters W.
Bioorg Med Chem Lett (2003) 13 : 4365 -4369
PubMed 14643327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.45 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341586 3 9.22
CHEMBL289228 TIPIFARNIB 3.0 1 9.05
CHEMBL343998 1 8.82
CHEMBL337751 3 8.77
CHEMBL140139 1 8.52
CHEMBL136633 1 8.30
CHEMBL335609 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341586 IC50 = 0.6 nM 9.22
CHEMBL289228 TIPIFARNIB IC50 = 0.9 nM 9.05
CHEMBL343998 IC50 = 1.5 nM 8.82
CHEMBL337751 IC50 = 1.7 nM 8.77
CHEMBL341586 IC50 = 2.5 nM 8.60
CHEMBL140139 IC50 = 3.0 nM 8.52
CHEMBL337751 IC50 = 3.5 nM 8.46
CHEMBL136633 IC50 = 5.0 nM 8.30
CHEMBL335609 IC50 = 7.0 nM 8.15
CHEMBL341586 IC50 = 22.0 nM 7.66
CHEMBL337751 IC50 = 36.0 nM 7.44