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Assay Detail

CHEMBL5115322

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

Binding
Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay
41
Total Activities
41
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

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 41 8.02 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208315 1 9.31
CHEMBL5206449 1 9.22
CHEMBL5182032 1 9.19
CHEMBL5200499 1 9.08
CHEMBL5179613 1 9.03
CHEMBL5187868 1 8.82
CHEMBL5193389 1 8.71
CHEMBL941 IMATINIB 4.0 1 8.55
CHEMBL5203239 1 8.51
CHEMBL5207040 1 8.50
CHEMBL5193726 1 8.46
CHEMBL5187601 1 8.32
CHEMBL5187489 1 8.26
CHEMBL5197019 1 8.23
CHEMBL5196374 1 8.16
CHEMBL5183302 1 8.16
CHEMBL5191144 1 8.07
CHEMBL5187532 1 8.06
CHEMBL5207617 1 8.03
CHEMBL5172694 1 8.03
CHEMBL5207653 1 7.98
CHEMBL5170705 1 7.98
CHEMBL5208081 1 7.84
CHEMBL5181452 1 7.83
CHEMBL5185114 1 7.82
CHEMBL5183677 1 7.81
CHEMBL5207090 1 7.76
CHEMBL5177033 1 7.66
CHEMBL5206184 1 7.63
CHEMBL5172580 1 7.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208315 IC50 = 0.49 nM 9.31
CHEMBL5206449 IC50 = 0.6 nM 9.22
CHEMBL5182032 IC50 = 0.65 nM 9.19
CHEMBL5200499 IC50 = 0.83 nM 9.08
CHEMBL5179613 IC50 = 0.94 nM 9.03
CHEMBL5187868 IC50 = 1.5 nM 8.82
CHEMBL5193389 IC50 = 1.94 nM 8.71
CHEMBL941 IMATINIB IC50 = 2.79 nM 8.55
CHEMBL5203239 IC50 = 3.11 nM 8.51
CHEMBL5207040 IC50 = 3.15 nM 8.50
CHEMBL5193726 IC50 = 3.45 nM 8.46
CHEMBL5187601 IC50 = 4.8 nM 8.32
CHEMBL5187489 IC50 = 5.53 nM 8.26
CHEMBL5197019 IC50 = 5.85 nM 8.23
CHEMBL5183302 IC50 = 6.99 nM 8.16
CHEMBL5196374 IC50 = 6.88 nM 8.16
CHEMBL5191144 IC50 = 8.6 nM 8.07
CHEMBL5187532 IC50 = 8.71 nM 8.06
CHEMBL5207617 IC50 = 9.45 nM 8.03
CHEMBL5172694 IC50 = 9.26 nM 8.03
CHEMBL5207653 IC50 = 10.37 nM 7.98
CHEMBL5170705 IC50 = 10.57 nM 7.98
CHEMBL5208081 IC50 = 14.47 nM 7.84
CHEMBL5181452 IC50 = 14.66 nM 7.83
CHEMBL5185114 IC50 = 15.0 nM 7.82
CHEMBL5183677 IC50 = 15.6 nM 7.81
CHEMBL5207090 IC50 = 17.45 nM 7.76
CHEMBL5177033 IC50 = 21.86 nM 7.66
CHEMBL5206184 IC50 = 23.45 nM 7.63
CHEMBL5172580 IC50 = 24.65 nM 7.61
CHEMBL5188615 IC50 = 27.08 nM 7.57
CHEMBL5176514 IC50 = 28.21 nM 7.55
CHEMBL5177838 IC50 = 29.2 nM 7.54
CHEMBL5194721 IC50 = 30.06 nM 7.52
CHEMBL5202743 IC50 = 41.5 nM 7.38
CHEMBL5203678 IC50 = 43.57 nM 7.36
CHEMBL5203127 IC50 = 49.99 nM 7.30
CHEMBL5189577 IC50 = 60.06 nM 7.22
CHEMBL5193797 IC50 = 60.64 nM 7.22
CHEMBL5172285 IC50 = 128.5 nM 6.89
CHEMBL5196757 IC50 = 201.51 nM 6.70