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Assay Detail

CHEMBL5127262

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

Binding
Inhibition of BLK (unknown origin)
4
Total Activities
4
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

Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.
Ran F, Liu Y, Wang C, Xu Z, Zhang Y, Liu Y, Zhao G, Ling Y.
Eur J Med Chem (2022) 229 : 114009 -114009
PubMed 34839996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.18 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 10.00
CHEMBL5193128 1 8.60
CHEMBL4071161 TIRABRUTINIB 4.0 1 5.95
CHEMBL5187554 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 0.1 nM 10.00
CHEMBL5193128 IC50 = 2.5 nM 8.60
CHEMBL4071161 TIRABRUTINIB IC50 = 1133.0 nM 5.95
CHEMBL5187554 IC50 > 1000.0 nM -