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Assay Detail

CHEMBL2185458

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Functional
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Publication

Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant.
Li Y, Shen M, Zhang Z, Luo J, Pan X, Lu X, Long H, Wen D, Zhang F, Leng F, Li Y, Tu Z, Ren X, Ding K, Ding K.
J Med Chem (2012) 55 : 10033 -10046
PubMed 23088644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.63 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 8.76
CHEMBL2177645 1 8.43
CHEMBL2178277 1 8.27
CHEMBL255863 NILOTINIB 4.0 1 7.06
CHEMBL941 IMATINIB 4.0 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 1.72 nM 8.76
CHEMBL2177645 IC50 = 3.73 nM 8.43
CHEMBL2178277 IC50 = 5.4 nM 8.27
CHEMBL255863 NILOTINIB IC50 = 87.2 nM 7.06
CHEMBL941 IMATINIB IC50 = 2377.0 nM 5.62