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Assay Detail

CHEMBL892514

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Binding
Inhibition of human Abl kinase expressed in Sf9 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives.
Horio T, Hamasaki T, Inoue T, Wakayama T, Itou S, Naito H, Asaki T, Hayase H, Niwa T.
Bioorg Med Chem Lett (2007) 17 : 2712 -2717
PubMed 17376680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.49 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203343 1 8.29
CHEMBL205723 1 8.06
CHEMBL536073 1 7.92
CHEMBL383010 1 7.92
CHEMBL206834 BAFETINIB 2.0 1 7.58
CHEMBL538337 1 7.50
CHEMBL205409 1 6.92
CHEMBL536983 1 6.85
CHEMBL941 IMATINIB 4.0 1 6.33
CHEMBL536753 1 -
CHEMBL203071 1 -
CHEMBL382605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203343 IC50 = 5.1 nM 8.29
CHEMBL205723 IC50 = 8.8 nM 8.06
CHEMBL536073 IC50 = 12.0 nM 7.92
CHEMBL383010 IC50 = 12.0 nM 7.92
CHEMBL206834 BAFETINIB IC50 = 26.0 nM 7.58
CHEMBL538337 IC50 = 32.0 nM 7.50
CHEMBL205409 IC50 = 120.0 nM 6.92
CHEMBL536983 IC50 = 140.0 nM 6.85
CHEMBL941 IMATINIB IC50 = 470.0 nM 6.33
CHEMBL536753 IC50 - -
CHEMBL203071 IC50 - -
CHEMBL382605 IC50 - -