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Assay Detail

CHEMBL5737487

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

Binding
KINOMEscan competition binding assay: This assay is described in https://www.discoverx.com/kinase-data-sheets/abl1-nonphosphorylated.
30
Total Activities
10
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
Kd 10 8.95 9.42
kon 10 - -
k_off 10 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5832508 3 9.42
CHEMBL5741416 3 9.40
CHEMBL386051 3 9.24
CHEMBL6019840 3 9.18
CHEMBL5960415 3 9.04
CHEMBL5757809 3 8.82
CHEMBL5936577 3 8.82
CHEMBL5908611 3 8.59
CHEMBL5812173 3 8.48
CHEMBL5926374 3 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5832508 Kd = 0.38 nM 9.42
CHEMBL5741416 Kd = 0.4 nM 9.40
CHEMBL386051 Kd = 0.58 nM 9.24
CHEMBL6019840 Kd = 0.66 nM 9.18
CHEMBL5960415 Kd = 0.91 nM 9.04
CHEMBL5757809 Kd = 1.5 nM 8.82
CHEMBL5936577 Kd = 1.5 nM 8.82
CHEMBL5908611 Kd = 2.6 nM 8.59
CHEMBL5812173 Kd = 3.3 nM 8.48
CHEMBL5926374 Kd = 3.5 nM 8.46
CHEMBL5908611 k_off = - s-1 -
CHEMBL5908611 kon = - -
CHEMBL5741416 k_off = - s-1 -
CHEMBL5741416 kon = - -
CHEMBL5812173 k_off = - s-1 -
CHEMBL5812173 kon = - -
CHEMBL5926374 k_off = - s-1 -
CHEMBL5926374 kon = - -
CHEMBL386051 k_off = - s-1 -
CHEMBL386051 kon = - -
CHEMBL5757809 kon = - -
CHEMBL5757809 k_off = - s-1 -
CHEMBL5936577 kon = - -
CHEMBL5936577 k_off = - s-1 -
CHEMBL5960415 kon = - -
CHEMBL5960415 k_off = - s-1 -
CHEMBL6019840 k_off = - s-1 -
CHEMBL6019840 kon = - -
CHEMBL5832508 kon = - -
CHEMBL5832508 k_off = - s-1 -