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Assay Detail

CHEMBL5342659

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

Binding
Inhibition of BTK in HEK293 cells using NanoGlo substrate incubated for 2 hrs by NanoBRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy.
Li YQ, Lannigan WG, Davoodi S, Daryaee F, Corrionero A, Alfonso P, Rodriguez-Santamaria JA, Wang N, Haley JD, Tonge PJ.
J Med Chem (2023) 66 : 7454 -7474
PubMed 37195170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.73 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065122 FENEBRUTINIB 3.0 1 7.92
CHEMBL5408743 1 7.01
CHEMBL5403472 1 6.50
CHEMBL5437508 1 5.50
CHEMBL43452 POMALIDOMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065122 FENEBRUTINIB IC50 = 12.1 nM 7.92
CHEMBL5408743 IC50 = 97.0 nM 7.01
CHEMBL5403472 IC50 = 320.0 nM 6.50
CHEMBL5437508 IC50 = 3200.0 nM 5.50
CHEMBL43452 POMALIDOMIDE IC50 - -