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Assay Detail

CHEMBL5124392

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

Binding
Inhibition of BTK (unknown origin)
7
Total Activities
7
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

Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
Sun SL, Wu SH, Kang JB, Ma YY, Chen L, Cao P, Chang L, Ding N, Xue X, Li NG, Shi ZH.
J Med Chem (2022) 65 : 7415 -7437
PubMed 35594541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.90 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4111143 1 9.70
CHEMBL4109377 1 9.70
CHEMBL5200336 1 9.52
CHEMBL5175002 1 8.96
CHEMBL4107779 1 8.85
CHEMBL5204333 1 7.97
CHEMBL3942924 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4111143 IC50 = 0.2 nM 9.70
CHEMBL4109377 IC50 = 0.2 nM 9.70
CHEMBL5200336 IC50 = 0.3 nM 9.52
CHEMBL5175002 IC50 = 1.1 nM 8.96
CHEMBL4107779 IC50 = 1.4 nM 8.85
CHEMBL5204333 IC50 = 10.7 nM 7.97
CHEMBL3942924 IC50 = 26.0 nM 7.58