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Assay Detail

CHEMBL4668367

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

Binding
Inhibition of wild type human ABL H396P mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assay
1
Total Activities
1
Compounds Tested
1
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

Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
Lu X,Smaill JB,Ding K
J Med Chem (2020) 63 : 10726 -10741
PubMed 32432477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.52 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171837 PONATINIB 4.0 1 9.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171837 PONATINIB IC50 = 0.3 nM 9.52