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Assay Detail

CHEMBL4818915

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

Binding
Inhibition of recombinant human TEC (174 to end residues) using EFPIYDFLPAKKK as substrate incubated for 40 mins in presence of [gamma33P]ATP by scintillation counting method
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 Tec (CHEMBL4246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
Tichenor MS, Wiener JJM, Rao NL, Pooley Deckhut C, Barbay JK, Kreutter KD, Bacani GM, Wei J, Chang L, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Seierstad M, Bembenek SD, Leonard KA, Lebsack AD, Venable JD, Edwards JP.
ACS Med Chem Lett (2021) 12 : 782 -790
PubMed 34055226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.39 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4851021 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4851021 IC50 = 409.0 nM 6.39