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Assay Detail

CHEMBL4714263

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

Binding
Inhibition of BTK (unknown origin) One-hour enzymatic assay without pre-incubation
5
Total Activities
5
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

Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.
Zheng J,Wu J,Ding X,Shen HC,Zou G
Bioorg Med Chem Lett (2021) 38 : 127862 -127862
PubMed 33609659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.74 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 9.30
CHEMBL4560385 1 9.30
CHEMBL3702854 RILZABRUTINIB 3.0 1 8.89
CHEMBL4163691 POSELTINIB 2.0 1 8.71
CHEMBL4594348 ELSUBRUTINIB 2.0 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 0.5 nM 9.30
CHEMBL4560385 IC50 = 0.5 nM 9.30
CHEMBL3702854 RILZABRUTINIB IC50 = 1.3 nM 8.89
CHEMBL4163691 POSELTINIB IC50 = 1.95 nM 8.71
CHEMBL4594348 ELSUBRUTINIB IC50 = 33.0 nM 7.48