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Assay Detail

CHEMBL5115323

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

Binding
Inhibition of Bcr-Abl T315I mutant (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay
ChEMBL ↗
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 6.63 7.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5183677 — — 1 7.61
CHEMBL5196374 — — 1 7.60
CHEMBL5193389 — — 1 7.50
CHEMBL5207653 — — 1 7.48
CHEMBL5206184 — — 1 7.22
CHEMBL5187532 — — 1 7.07
CHEMBL5208315 — — 1 6.96
CHEMBL5172580 — — 1 6.96
CHEMBL941 IMATINIB 4.0 1 6.94
CHEMBL5207617 — — 1 6.93
CHEMBL5176514 — — 1 6.92
CHEMBL5179613 — — 1 6.90
CHEMBL5193726 — — 1 6.89
CHEMBL5207040 — — 1 6.87
CHEMBL5172694 — — 1 6.86
CHEMBL5185114 — — 1 6.86
CHEMBL5187489 — — 1 6.84
CHEMBL5177033 — — 1 6.82
CHEMBL5183302 — — 1 6.77
CHEMBL5188615 — — 1 6.75
CHEMBL5187868 — — 1 6.72
CHEMBL5206449 — — 1 6.72
CHEMBL5200499 — — 1 6.70
CHEMBL5203127 — — 1 6.62
CHEMBL5208081 — — 1 6.58
CHEMBL5203239 — — 1 6.52
CHEMBL5203678 — — 1 6.51
CHEMBL5182032 — — 1 6.47
CHEMBL5197019 — — 1 6.46
CHEMBL5177838 — — 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5183677 — IC50 = 24.69 nM 7.61
CHEMBL5196374 — IC50 = 25.21 nM 7.60
CHEMBL5193389 — IC50 = 31.55 nM 7.50
CHEMBL5207653 — IC50 = 33.28 nM 7.48
CHEMBL5206184 — IC50 = 59.62 nM 7.22
CHEMBL5187532 — IC50 = 84.82 nM 7.07
CHEMBL5208315 — IC50 = 110.85 nM 6.96
CHEMBL5172580 — IC50 = 109.91 nM 6.96
CHEMBL941 IMATINIB IC50 = 115.64 nM 6.94
CHEMBL5207617 — IC50 = 118.09 nM 6.93
CHEMBL5176514 — IC50 = 121.01 nM 6.92
CHEMBL5179613 — IC50 = 125.08 nM 6.90
CHEMBL5193726 — IC50 = 127.31 nM 6.89
CHEMBL5207040 — IC50 = 135.44 nM 6.87
CHEMBL5185114 — IC50 = 137.08 nM 6.86
CHEMBL5172694 — IC50 = 139.64 nM 6.86
CHEMBL5187489 — IC50 = 143.87 nM 6.84
CHEMBL5177033 — IC50 = 150.0 nM 6.82
CHEMBL5183302 — IC50 = 169.14 nM 6.77
CHEMBL5188615 — IC50 = 178.39 nM 6.75
CHEMBL5187868 — IC50 = 188.4 nM 6.72
CHEMBL5206449 — IC50 = 189.79 nM 6.72
CHEMBL5200499 — IC50 = 199.86 nM 6.70
CHEMBL5203127 — IC50 = 236.97 nM 6.62
CHEMBL5208081 — IC50 = 261.14 nM 6.58
CHEMBL5203239 — IC50 = 302.82 nM 6.52
CHEMBL5203678 — IC50 = 309.78 nM 6.51
CHEMBL5182032 — IC50 = 337.78 nM 6.47
CHEMBL5197019 — IC50 = 343.19 nM 6.46
CHEMBL5177838 — IC50 = 348.79 nM 6.46
CHEMBL5187601 — IC50 = 388.49 nM 6.41
CHEMBL5181452 — IC50 = 410.26 nM 6.39
CHEMBL5207090 — IC50 = 487.02 nM 6.31
CHEMBL5170705 — IC50 = 667.22 nM 6.18
CHEMBL5189577 — IC50 = 800.95 nM 6.10
CHEMBL5194721 — IC50 = 1342.81 nM 5.87
CHEMBL5172285 — IC50 = 1589.62 nM 5.80
CHEMBL5193797 — IC50 = 1878.0 nM 5.73
CHEMBL5196757 — IC50 = 1892.0 nM 5.72
CHEMBL5202743 — IC50 = 3443.3 nM 5.46
CHEMBL5191144 — IC50 = 3667.06 nM 5.44