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Assay Detail

CHEMBL5716031

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

Binding
Inhibition of human Itk using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay
3
Total Activities
3
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase ITK/TSK (CHEMBL2959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Itk inhibitors block T-cell activation and murine lung inflammation.
Lin TA, McIntyre KW, Das J, Liu C, O'Day KD, Penhallow B, Hung CY, Whitney GS, Shuster DJ, Yang X, Townsend R, Postelnek J, Spergel SH, Lin J, Moquin RV, Furch JA, Kamath AV, Zhang H, Marathe PH, Perez-Villar JJ, Doweyko A, Killar L, Dodd JH, Barrish JC, Wityak J, Kanner SB.
Biochemistry (2004) 43 : 11056 -11062
PubMed 15323564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.91 7.72

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0005140
EFO_ID EFO_ID - HP:0002099
EFO_TERM EFO_TERM - autoimmune disease
EFO_TERM EFO_TERM - asthma

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209148 1 7.72
CHEMBL382362 1 7.02
CHEMBL205799 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209148 IC50 = 19.0 nM 7.72
CHEMBL382362 IC50 = 96.0 nM 7.02
CHEMBL205799 IC50 = 1000.0 nM 6.00