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Assay Detail

CHEMBL5342676

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

Functional
Cytotoxicity against human MINO cells incubated for 48 hrs by celltitre glo 2.0 assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MINO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6 7.90 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5408743 1 8.66
CHEMBL4065122 FENEBRUTINIB 3.0 1 8.11
CHEMBL4450122 1 7.98
CHEMBL4754443 1 7.96
CHEMBL43452 POMALIDOMIDE 4.0 1 7.68
CHEMBL4441907 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5408743 IC50 = 2.2 nM 8.66
CHEMBL4065122 FENEBRUTINIB IC50 = 7.8 nM 8.11
CHEMBL4450122 IC50 = 10.4 nM 7.98
CHEMBL4754443 IC50 = 10.9 nM 7.96
CHEMBL43452 POMALIDOMIDE IC50 = 20.8 nM 7.68
CHEMBL4441907 IC50 = 100.0 nM 7.00