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Assay Detail

CHEMBL4152874

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

Binding
Inhibition of BTK (unknown origin)
12
Total Activities
12
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

The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
Liang C, Tian D, Ren X, Ding S, Jia M, Xin M, Thareja S.
Eur J Med Chem (2018) 151 : 315 -326
PubMed 29631132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.39 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3301625 SPEBRUTINIB 2.0 1 9.15
CHEMBL3979355 1 8.89
CHEMBL3702836 1 8.72
CHEMBL1230541 1 8.72
CHEMBL4172284 1 8.70
CHEMBL4175428 1 8.66
CHEMBL3707348 ACALABRUTINIB 4.0 1 8.52
CHEMBL4167139 1 8.40
CHEMBL2057918 1 8.40
CHEMBL4162057 1 8.23
CHEMBL3263640 1 8.10
CHEMBL4163691 POSELTINIB 2.0 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3301625 SPEBRUTINIB IC50 = 0.7 nM 9.15
CHEMBL3979355 IC50 = 1.3 nM 8.89
CHEMBL3702836 IC50 = 1.9 nM 8.72
CHEMBL1230541 IC50 = 1.9 nM 8.72
CHEMBL4172284 IC50 = 2.0 nM 8.70
CHEMBL4175428 IC50 = 2.2 nM 8.66
CHEMBL3707348 ACALABRUTINIB IC50 = 3.0 nM 8.52
CHEMBL4167139 IC50 = 4.0 nM 8.40
CHEMBL2057918 IC50 = 4.0 nM 8.40
CHEMBL4162057 IC50 = 5.9 nM 8.23
CHEMBL3263640 IC50 = 8.0 nM 8.10
CHEMBL4163691 POSELTINIB IC50 = 651.95 nM 6.19