Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3810822

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

Binding
Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.
Daydé-Cazals B, Fauvel B, Singer M, Feneyrolles C, Bestgen B, Gassiot F, Spenlinhauer A, Warnault P, Van Hijfte N, Borjini N, Chevé G, Yasri A.
J Med Chem (2016) 59 : 3886 -3905
PubMed 27010810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 9.64 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3808884 1 10.40
CHEMBL5416410 DASATINIB 4.0 1 10.40
CHEMBL1171837 PONATINIB 4.0 1 10.30
CHEMBL941 IMATINIB 4.0 1 7.47
CHEMBL553 ERLOTINIB 4.0 1 -
CHEMBL535 SUNITINIB 4.0 1 -
CHEMBL1336 SORAFENIB 4.0 1 -
CHEMBL1173655 AFATINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3808884 EC50 = 0.04 nM 10.40
CHEMBL5416410 DASATINIB EC50 = 0.04 nM 10.40
CHEMBL1171837 PONATINIB EC50 = 0.05 nM 10.30
CHEMBL941 IMATINIB EC50 = 34.0 nM 7.47
CHEMBL553 ERLOTINIB EC50 - -
CHEMBL535 SUNITINIB EC50 - -
CHEMBL1336 SORAFENIB EC50 - -
CHEMBL1173655 AFATINIB EC50 - -