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Assay Detail

CHEMBL4182608

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

Binding
Inhibition of BTK (unknown origin) using FITC-labeled Srctide substrate and ATP by microfluidic mobility shift assay
6
Total Activities
6
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

Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.
Kawahata W, Asami T, Irie T, Sawa M.
Bioorg Med Chem Lett (2018) 28 : 145 -151
PubMed 29198867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.07 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211270 1 8.21
CHEMBL4203409 1 8.05
CHEMBL4212308 1 7.40
CHEMBL4208579 1 7.28
CHEMBL4205977 1 6.36
CHEMBL4217692 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211270 IC50 = 6.1 nM 8.21
CHEMBL4203409 IC50 = 9.0 nM 8.05
CHEMBL4212308 IC50 = 40.0 nM 7.40
CHEMBL4208579 IC50 = 52.0 nM 7.28
CHEMBL4205977 IC50 = 440.0 nM 6.36
CHEMBL4217692 IC50 = 7300.0 nM 5.14