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Assay Detail

CHEMBL4726209

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

Binding
Inhibition of recombinant full length human His-tagged BLK cytoplasmic domain expressed in baculovirus expression system using tyrosine-1 peptide as substrate preincubated for 1 hr in presence of ATP by Z'-LYTE assay
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 Blk (CHEMBL2250)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of quinoline-based irreversible BTK inhibitors.
de Bruin G,Demont D,de Zwart E,Verkaik S,Hoogenboom N,van de Kar B,van Lith B,Emmelot-van Hoek M,Gulrajani M,Covey T,Kaptein A,Barf T
Bioorg Med Chem Lett (2020) 30 : 127261 -127261
PubMed 32527559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.22 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 10.00
CHEMBL4755977 1 8.08
CHEMBL4752700 1 7.67
CHEMBL4782725 1 7.14
CHEMBL3707348 ACALABRUTINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 0.1 nM 10.00
CHEMBL4755977 IC50 = 8.3 nM 8.08
CHEMBL4752700 IC50 = 21.2 nM 7.67
CHEMBL4782725 IC50 = 72.0 nM 7.14
CHEMBL3707348 ACALABRUTINIB IC50 > 1000.0 nM -