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Assay Detail

CHEMBL3267592

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

Binding
Inhibition of ITK in human Jurkat cells assessed as decrease in phosphorylation of PLC-gamma1 by immunodetection assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.
Pastor RM, Burch JD, Magnuson S, Ortwine DF, Chen Y, De La Torre K, Ding X, Eigenbrot C, Johnson A, Liimatta M, Liu Y, Shia S, Wang X, Wu LC, Pei Z.
Bioorg Med Chem Lett (2014) 24 : 2448 -2452
PubMed 24767842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.53 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3263055 1 7.36
CHEMBL3263053 1 6.76
CHEMBL3263036 1 6.64
CHEMBL3262780 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3263055 IC50 = 44.0 nM 7.36
CHEMBL3263053 IC50 = 173.0 nM 6.76
CHEMBL3263036 IC50 = 231.0 nM 6.64
CHEMBL3262780 IC50 = 4600.0 nM 5.34