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Assay Detail

CHEMBL4819975

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

Binding
Inhibition of human BTK using poly (Glu,Tyr) as substrate in presence of ATP and Ci(gamma33-P) ATP measured by microplate reader assay
14
Total Activities
14
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

1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase.
Krajčovičová S, Jorda R, Vanda D, Soural M, Kryštof V.
Eur J Med Chem (2021) 211 : 113094 -113094
PubMed 33340912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.90 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3647964 1 7.72
CHEMBL4858294 1 7.60
CHEMBL4865664 1 7.57
CHEMBL4875035 1 7.46
CHEMBL4852342 1 7.39
CHEMBL4873565 1 7.10
CHEMBL4867619 1 6.81
CHEMBL4852053 1 6.78
CHEMBL4879055 1 6.58
CHEMBL4855825 1 6.28
CHEMBL4859682 1 6.26
CHEMBL4868893 1 6.15
CHEMBL4869977 1 6.03
CHEMBL4854403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3647964 IC50 = 19.0 nM 7.72
CHEMBL4858294 IC50 = 25.0 nM 7.60
CHEMBL4865664 IC50 = 27.0 nM 7.57
CHEMBL4875035 IC50 = 35.0 nM 7.46
CHEMBL4852342 IC50 = 41.0 nM 7.39
CHEMBL4873565 IC50 = 79.0 nM 7.10
CHEMBL4867619 IC50 = 155.0 nM 6.81
CHEMBL4852053 IC50 = 166.0 nM 6.78
CHEMBL4879055 IC50 = 264.0 nM 6.58
CHEMBL4855825 IC50 = 527.0 nM 6.28
CHEMBL4859682 IC50 = 545.0 nM 6.26
CHEMBL4868893 IC50 = 709.0 nM 6.15
CHEMBL4869977 IC50 = 932.0 nM 6.03
CHEMBL4854403 IC50 > 10000.0 nM -