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Assay Detail

CHEMBL4721776

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

Binding
Binding affinity to human LCK using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase 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 Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift.
Dart ML,Machleidt T,Jost E,Schwinn MK,Robers MB,Shi C,Kirkland TA,Killoran MP,Wilkinson JM,Hartnett JR,Zimmerman K,Wood KV
ACS Med Chem Lett (2018) 9 : 546 -551
PubMed 29937980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.55 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171837 PONATINIB 4.0 1 9.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171837 PONATINIB IC50 = 0.28 nM 9.55