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Assay Detail

CHEMBL749697

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

Functional
T24H-ras-transformed NIH3T3 cell proliferation
12
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 1 — Organism
Curated By Expert

Target

NIH3T3 (CHEMBL614822)
Type CELL-LINE
Organism Mus musculus

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 12 7.48 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289228 TIPIFARNIB 3.0 1 8.77
CHEMBL341586 3 8.00
CHEMBL343998 1 7.76
CHEMBL337751 3 7.70
CHEMBL335609 1 7.55
CHEMBL136633 1 7.06
CHEMBL140139 1 6.73
CHEMBL343060 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289228 TIPIFARNIB IC50 = 1.7 nM 8.77
CHEMBL341586 IC50 = 10.0 nM 8.00
CHEMBL341586 IC50 = 12.0 nM 7.92
CHEMBL343998 IC50 = 17.5 nM 7.76
CHEMBL337751 IC50 = 20.0 nM 7.70
CHEMBL335609 IC50 = 28.0 nM 7.55
CHEMBL337751 IC50 = 55.0 nM 7.26
CHEMBL136633 IC50 = 88.0 nM 7.06
CHEMBL341586 IC50 = 108.0 nM 6.97
CHEMBL140139 IC50 = 186.0 nM 6.73
CHEMBL343060 IC50 = 304.0 nM 6.52
CHEMBL337751 IC50 > 500.0 nM -