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Assay Detail

CHEMBL750685

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Functional
In vitro inhibition of NIH3T3 cell proliferation
8
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

4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA.
Angibaud P, Saha AK, Bourdrez X, End DW, Freyne E, Lezouret P, Mannens G, Mevellec L, Meyer C, Pilatte I, Poncelet V, Roux B, Smets G, Van Dun J, Venet M, Wouters W.
Bioorg Med Chem Lett (2003) 13 : 4361 -4364
PubMed 14643326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.33 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289228 TIPIFARNIB 3.0 1 8.77
CHEMBL343172 1 7.92
CHEMBL136831 1 7.62
CHEMBL137087 1 7.24
CHEMBL342827 1 7.10
CHEMBL344642 1 6.82
CHEMBL342254 1 6.76
CHEMBL344703 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289228 TIPIFARNIB IC50 = 1.7 nM 8.77
CHEMBL343172 IC50 = 12.0 nM 7.92
CHEMBL136831 IC50 = 24.0 nM 7.62
CHEMBL137087 IC50 = 58.0 nM 7.24
CHEMBL342827 IC50 = 80.0 nM 7.10
CHEMBL344642 IC50 = 151.0 nM 6.82
CHEMBL342254 IC50 = 174.0 nM 6.76
CHEMBL344703 IC50 = 400.0 nM 6.40