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Assay Detail

CHEMBL3267591

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

Binding
Inhibition of full-length ITK (unknown origin) using biotin-EQEDEPEGIYGVLF-NH2 as substrate by plate reader analysis
25
Total Activities
25
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 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
Ki 25 8.19 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3263053 1 10.00
CHEMBL3263055 1 9.64
CHEMBL3263050 1 9.25
CHEMBL3263036 1 9.10
CHEMBL3263054 1 9.10
CHEMBL3263052 1 9.03
CHEMBL3263049 1 9.00
CHEMBL3263035 1 8.85
CHEMBL3263039 1 8.77
CHEMBL3263038 1 8.47
CHEMBL3263051 1 8.18
CHEMBL3263037 1 8.11
CHEMBL3262783 1 8.00
CHEMBL3263044 1 7.96
CHEMBL3262780 1 7.82
CHEMBL3263046 1 7.57
CHEMBL3263047 1 7.46
CHEMBL3263045 1 7.44
CHEMBL3263048 1 7.36
CHEMBL3263043 1 7.28
CHEMBL3262782 1 7.23
CHEMBL3263042 1 6.42
CHEMBL3262781 1 6.24
CHEMBL3263041 1 -
CHEMBL3263040 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3263053 Ki = 0.1 nM 10.00
CHEMBL3263055 Ki = 0.23 nM 9.64
CHEMBL3263050 Ki = 0.56 nM 9.25
CHEMBL3263036 Ki = 0.8 nM 9.10
CHEMBL3263054 Ki = 0.8 nM 9.10
CHEMBL3263052 Ki = 0.93 nM 9.03
CHEMBL3263049 Ki = 1.0 nM 9.00
CHEMBL3263035 Ki = 1.4 nM 8.85
CHEMBL3263039 Ki = 1.7 nM 8.77
CHEMBL3263038 Ki = 3.4 nM 8.47
CHEMBL3263051 Ki = 6.6 nM 8.18
CHEMBL3263037 Ki = 7.8 nM 8.11
CHEMBL3262783 Ki = 10.0 nM 8.00
CHEMBL3263044 Ki = 11.0 nM 7.96
CHEMBL3262780 Ki = 15.0 nM 7.82
CHEMBL3263046 Ki = 27.0 nM 7.57
CHEMBL3263047 Ki = 35.0 nM 7.46
CHEMBL3263045 Ki = 36.0 nM 7.44
CHEMBL3263048 Ki = 44.0 nM 7.36
CHEMBL3263043 Ki = 53.0 nM 7.28
CHEMBL3262782 Ki = 59.0 nM 7.23
CHEMBL3263042 Ki = 381.0 nM 6.42
CHEMBL3262781 Ki = 580.0 nM 6.24
CHEMBL3263041 Ki > 4.0 nM -
CHEMBL3263040 Ki > 4.0 nM -