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Assay Detail

CHEMBL4818909

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

Binding
Inhibition of BTK in C57Bl/6 mouse splenocyte assessed as reduction in anti-IgM-induced CD69 expression incubated for 1 hr followed anti-IgM stimulation and measured after overnight by flow cytometry analysis
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Splenocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL3259478)
Type SINGLE PROTEIN
Organism Mus musculus

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 15 7.53 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852459 1 8.12
CHEMBL4846828 1 8.10
CHEMBL4851021 1 7.96
CHEMBL4875401 1 7.89
CHEMBL4853403 2 7.72
CHEMBL4854911 1 7.70
CHEMBL4871745 1 7.52
CHEMBL4871385 1 7.38
CHEMBL4849068 1 7.10
CHEMBL4861899 1 6.89
CHEMBL4873622 1 -
CHEMBL4877611 1 -
CHEMBL4877368 1 -
CHEMBL4863521 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852459 IC50 = 7.6 nM 8.12
CHEMBL4846828 IC50 = 7.9 nM 8.10
CHEMBL4851021 IC50 = 11.0 nM 7.96
CHEMBL4875401 IC50 = 13.0 nM 7.89
CHEMBL4853403 IC50 = 19.0 nM 7.72
CHEMBL4854911 IC50 = 20.0 nM 7.70
CHEMBL4871745 IC50 = 30.0 nM 7.52
CHEMBL4871385 IC50 = 42.0 nM 7.38
CHEMBL4849068 IC50 = 80.0 nM 7.10
CHEMBL4861899 IC50 = 130.0 nM 6.89
CHEMBL4853403 IC50 = 400.0 nM 6.40
CHEMBL4873622 IC50 - -
CHEMBL4877611 IC50 - -
CHEMBL4877368 IC50 - -
CHEMBL4863521 IC50 - -