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Assay Detail

CHEMBL5115329

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Functional
Antiproliferative activity against human K-562R cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K-562R
Confidence 1 — Organism
Curated By Autocuration

Target

K-562R (CHEMBL4296447)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of trizole-based heteroaromatic derivatives as Bcr-Abl kinase inhibitors.
Pan X, Liu N, Liu Y, Zhang Q, Wang K, Liu X, Zhang J.
Eur J Med Chem (2022) 238 : 114425 -114425
PubMed 35561654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.23 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171837 PONATINIB 4.0 1 7.10
CHEMBL5206449 1 5.72
CHEMBL5208315 1 4.88
CHEMBL5187868 1 4.40
CHEMBL941 IMATINIB 4.0 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171837 PONATINIB IC50 = 80.0 nM 7.10
CHEMBL5206449 IC50 = 1910.0 nM 5.72
CHEMBL5208315 IC50 = 13350.0 nM 4.88
CHEMBL5187868 IC50 = 40140.0 nM 4.40
CHEMBL941 IMATINIB IC50 = 93010.0 nM 4.03