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Assay Detail

CHEMBL3420415

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

Binding
Inhibition of GST-fused Zap70 (unknown origin) expressed in insect SF9 cells using biotin-EQEDEPEGDYFEWLE-CONH2 as substrate preincubated for 10 mins followed by substrate/ATP addition measured after 45 mins by TR-FRET assay
1
Total Activities
1
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 Autocuration

Target

Tyrosine-protein kinase ZAP-70 (CHEMBL2803)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Ellis JM, Altman MD, Bass A, Butcher JW, Byford AJ, Donofrio A, Galloway S, Haidle AM, Jewell J, Kelly N, Leccese EK, Lee S, Maddess M, Miller JR, Moy LY, Osimboni E, Otte RD, Reddy MV, Spencer K, Sun B, Vincent SH, Ward GJ, Woo GH, Yang C, Houshyar H, Northrup AB.
J Med Chem (2015) 58 : 1929 -1939
PubMed 25625541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.28 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3415583 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3415583 IC50 = 5.3 nM 8.28