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Assay Detail

CHEMBL914489

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Functional
Antiproliferative activity against human WiDr cells after 72 hrs
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type WiDr
Confidence 1 — Organism
Curated By Autocuration

Target

WiDr (CHEMBL614647)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen ML, Wityak J, Borzilleri RM.
J Med Chem (2004) 47 : 6658 -6661
PubMed 15615512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.33 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424906 1 8.39
CHEMBL385698 1 8.10
CHEMBL222218 1 7.64
CHEMBL214617 1 7.57
CHEMBL217039 1 7.57
CHEMBL273250 1 7.50
CHEMBL216240 1 7.39
CHEMBL5416410 DASATINIB 4.0 1 7.28
CHEMBL222036 1 6.75
CHEMBL386118 1 6.68
CHEMBL187697 1 6.57
CHEMBL189649 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424906 IC50 = 4.1 nM 8.39
CHEMBL385698 IC50 = 7.9 nM 8.10
CHEMBL222218 IC50 = 23.0 nM 7.64
CHEMBL214617 IC50 = 27.0 nM 7.57
CHEMBL217039 IC50 = 27.0 nM 7.57
CHEMBL273250 IC50 = 32.0 nM 7.50
CHEMBL216240 IC50 = 41.0 nM 7.39
CHEMBL5416410 DASATINIB IC50 = 52.0 nM 7.28
CHEMBL222036 IC50 = 180.0 nM 6.75
CHEMBL386118 IC50 = 210.0 nM 6.68
CHEMBL187697 IC50 = 270.0 nM 6.57
CHEMBL189649 IC50 = 270.0 nM 6.57