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Assay Detail

CHEMBL4036726

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

Binding
Inhibition of BTK in human monocytes assessed as inhibition of FCgammaR activation-induced TNFalpha production by ELISA
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 BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
Wang X, Barbosa J, Blomgren P, Bremer MC, Chen J, Crawford JJ, Deng W, Dong L, Eigenbrot C, Gallion S, Hau J, Hu H, Johnson AR, Katewa A, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, DiPaolo J, Reif K, Scheerens H, Schmitt A, Wong H, Xiong JM, Xu J, Zhao Z, Zhou F, Currie KS, Young WB.
ACS Med Chem Lett (2017) 8 : 608 -613
PubMed 28626519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.48 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3670082 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3670082 EC50 = 33.0 nM 7.48