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Assay Detail

CHEMBL2351848

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Functional
Cytotoxicity against mouse BA/F3 cells transfected with Bcr-Abl T315I mutant after 48 hrs by XTT assay
13
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant.
Hong S, Kim J, Yun SM, Lee H, Park Y, Hong SS, Hong S.
J Med Chem (2013) 56 : 3531 -3545
PubMed 23600806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.20 7.11
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347725 1 7.11
CHEMBL2347723 1 6.85
CHEMBL2347722 2 6.54
CHEMBL2347724 1 6.54
CHEMBL2347731 1 6.39
CHEMBL2347728 1 6.25
CHEMBL2347729 1 6.06
CHEMBL2347726 1 5.96
CHEMBL2347727 1 5.87
CHEMBL2347730 1 5.84
CHEMBL2347710 1 5.67
CHEMBL941 IMATINIB 4.0 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347725 IC50 = 78.0 nM 7.11
CHEMBL2347723 IC50 = 140.0 nM 6.85
CHEMBL2347724 IC50 = 290.0 nM 6.54
CHEMBL2347722 IC50 = 290.0 nM 6.54
CHEMBL2347731 IC50 = 410.0 nM 6.39
CHEMBL2347728 IC50 = 560.0 nM 6.25
CHEMBL2347729 IC50 = 870.0 nM 6.06
CHEMBL2347726 IC50 = 1090.0 nM 5.96
CHEMBL2347727 IC50 = 1350.0 nM 5.87
CHEMBL2347730 IC50 = 1440.0 nM 5.84
CHEMBL2347710 IC50 = 2140.0 nM 5.67
CHEMBL941 IMATINIB IC50 = 4790.0 nM 5.32
CHEMBL2347722 Inhibition - % -