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Assay Detail

CHEMBL4385494

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

Binding
Inhibition of BTK in human whole blood assessed as reduction in anti-human IgE antibody-stimulated histamine release pretreated for 2 hrs followed by anti-human IgE antibody-stimulation and measured after 30 mins by ELISA
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.
Schnute ME, Benoit SE, Buchler IP, Caspers N, Grapperhaus ML, Han S, Hotchandani R, Huang N, Hughes RO, Juba BM, Kim KH, Liu E, McCarthy E, Messing D, Miyashiro JS, Mohan S, O'Connell TN, Ohren JF, Parikh MD, Schmidt M, Selness SR, Springer JR, Thanabal V, Trujillo JI, Walker DP, Wan ZK, Withka JM, Wittwer AJ, Wood NL, Xing L, Zapf CW, Douhan J.
ACS Med Chem Lett (2019) 10 : 80 -85
PubMed 30655951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.31 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456283 1 7.68
CHEMBL4456974 1 7.38
CHEMBL4462332 1 7.30
CHEMBL4560385 1 7.19
CHEMBL4469663 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456283 IC50 = 21.0 nM 7.68
CHEMBL4456974 IC50 = 42.0 nM 7.38
CHEMBL4462332 IC50 = 50.0 nM 7.30
CHEMBL4560385 IC50 = 64.0 nM 7.19
CHEMBL4469663 IC50 = 95.0 nM 7.02