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Assay Detail

CHEMBL5242619

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

Binding
Irreversible inhibition of BTK (unknown origin)
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

Progress in the development of small molecular inhibitors of the Bruton's tyrosine kinase (BTK) as a promising cancer therapy.
Liu XJ, Xu-Liu, Pang XJ, -Ying Yuan X, Yu GX, Li YR, Guan YF, Zhang YB, Song J, Zhang QR, Zhang SY.
Bioorg Med Chem (2021) 47 : 116358 -116358
PubMed 34479103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.96 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5275119 1 9.30
CHEMBL1873475 IBRUTINIB 4.0 1 9.30
CHEMBL3301625 SPEBRUTINIB 2.0 1 9.15
CHEMBL4650321 ORELABRUTINIB 3.0 1 8.80
CHEMBL5285357 1 8.66
CHEMBL3707348 ACALABRUTINIB 4.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5275119 IC50 = 0.5 nM 9.30
CHEMBL1873475 IBRUTINIB IC50 = 0.5 nM 9.30
CHEMBL3301625 SPEBRUTINIB IC50 = 0.7 nM 9.15
CHEMBL4650321 ORELABRUTINIB IC50 = 1.6 nM 8.80
CHEMBL5285357 IC50 = 2.2 nM 8.66
CHEMBL3707348 ACALABRUTINIB IC50 = 3.0 nM 8.52