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Assay Detail

CHEMBL5108965

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of BCR-ABL (unknown origin)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Bcr/Abl fusion protein (CHEMBL2096618)
Type CHIMERIC PROTEIN
Organism Homo sapiens

Publication

The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
Pan YL, Zeng SX, Hao RR, Liang MH, Shen ZR, Huang WH.
Eur J Med Chem (2022) 238 : 114442 -114442
PubMed 35551036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.53 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255863 NILOTINIB 4.0 1 9.00
CHEMBL4297524 RADOTINIB 3.0 1 8.92
CHEMBL288441 BOSUTINIB 4.0 1 8.85
CHEMBL384575 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255863 NILOTINIB IC50 = 1.0 nM 9.00
CHEMBL4297524 RADOTINIB IC50 = 1.2 nM 8.92
CHEMBL288441 BOSUTINIB IC50 = 1.4 nM 8.85
CHEMBL384575 IC50 = 47.0 nM 7.33