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Assay Detail

CHEMBL923928

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

Binding
Inhibition of Abl
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Tyrosine-protein kinase ABL1 (CHEMBL1862)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.
Cao J, Fine R, Gritzen C, Hood J, Kang X, Klebansky B, Lohse D, Mak CC, McPherson A, Noronha G, Palanki MS, Pathak VP, Renick J, Soll R, Zeng B, Zhu H.
Bioorg Med Chem Lett (2007) 17 : 5812 -5818
PubMed 17827012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 8.51 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250213 1 10.21
CHEMBL250019 1 9.52
CHEMBL250021 1 9.40
CHEMBL399246 1 9.30
CHEMBL398279 1 9.00
CHEMBL400402 1 8.89
CHEMBL250821 1 8.89
CHEMBL250214 1 8.77
CHEMBL399268 1 8.77
CHEMBL400403 1 8.59
CHEMBL250218 1 8.54
CHEMBL249821 1 8.52
CHEMBL440963 1 8.47
CHEMBL250625 1 8.46
CHEMBL398845 1 8.46
CHEMBL249819 1 8.38
CHEMBL250623 1 8.36
CHEMBL231220 1 8.30
CHEMBL250423 1 8.29
CHEMBL249820 1 8.11
CHEMBL436137 1 7.96
CHEMBL231524 1 7.80
CHEMBL230686 1 7.70
CHEMBL251015 1 7.62
CHEMBL400303 1 7.57
CHEMBL268825 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250213 Ki = 0.062 nM 10.21
CHEMBL250019 Ki = 0.3 nM 9.52
CHEMBL250021 Ki = 0.4 nM 9.40
CHEMBL399246 Ki = 0.5 nM 9.30
CHEMBL398279 Ki = 1.0 nM 9.00
CHEMBL400402 Ki = 1.3 nM 8.89
CHEMBL250821 Ki = 1.3 nM 8.89
CHEMBL250214 Ki = 1.7 nM 8.77
CHEMBL399268 Ki = 1.7 nM 8.77
CHEMBL400403 Ki = 2.6 nM 8.59
CHEMBL250218 Ki = 2.9 nM 8.54
CHEMBL249821 Ki = 3.0 nM 8.52
CHEMBL440963 Ki = 3.4 nM 8.47
CHEMBL250625 Ki = 3.5 nM 8.46
CHEMBL398845 Ki = 3.5 nM 8.46
CHEMBL249819 Ki = 4.2 nM 8.38
CHEMBL250623 Ki = 4.4 nM 8.36
CHEMBL231220 Ki = 5.0 nM 8.30
CHEMBL250423 Ki = 5.1 nM 8.29
CHEMBL249820 Ki = 7.7 nM 8.11
CHEMBL436137 Ki = 11.0 nM 7.96
CHEMBL231524 Ki = 16.0 nM 7.80
CHEMBL230686 Ki = 20.0 nM 7.70
CHEMBL251015 Ki = 24.0 nM 7.62
CHEMBL400303 Ki = 27.0 nM 7.57
CHEMBL268825 Ki = 42.0 nM 7.38