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Assay Detail

CHEMBL5737488

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

Binding
Z'-LITE biochemical assay: IC50 against Abelson kinase ABL1 was determined by Life Technologies corporation though the Z′-LITE biochemical assay.
27
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Functionalized pyrano[2,3-D]pyrimidin-7-one derivatives and methods for their preparation and use
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.13 8.90
kon 9 - -
k_off 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5832508 3 8.90
CHEMBL6019840 3 8.68
CHEMBL5741416 3 8.67
CHEMBL5960415 3 8.46
CHEMBL5936577 3 7.80
CHEMBL5757809 3 7.79
CHEMBL5926374 3 7.76
CHEMBL5812173 3 7.73
CHEMBL5908611 3 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5832508 IC50 = 1.27 nM 8.90
CHEMBL6019840 IC50 = 2.09 nM 8.68
CHEMBL5741416 IC50 = 2.13 nM 8.67
CHEMBL5960415 IC50 = 3.51 nM 8.46
CHEMBL5936577 IC50 = 15.7 nM 7.80
CHEMBL5757809 IC50 = 16.1 nM 7.79
CHEMBL5926374 IC50 = 17.5 nM 7.76
CHEMBL5812173 IC50 = 18.7 nM 7.73
CHEMBL5908611 IC50 = 42.6 nM 7.37
CHEMBL5926374 kon = - -
CHEMBL5926374 k_off = - s-1 -
CHEMBL5812173 kon = - -
CHEMBL5812173 k_off = - s-1 -
CHEMBL5741416 kon = - -
CHEMBL5741416 k_off = - s-1 -
CHEMBL5908611 kon = - -
CHEMBL5908611 k_off = - s-1 -
CHEMBL5757809 k_off = - s-1 -
CHEMBL5936577 kon = - -
CHEMBL6019840 k_off = - s-1 -
CHEMBL6019840 kon = - -
CHEMBL5832508 k_off = - s-1 -
CHEMBL5832508 kon = - -
CHEMBL5960415 k_off = - s-1 -
CHEMBL5960415 kon = - -
CHEMBL5757809 kon = - -
CHEMBL5936577 k_off = - s-1 -