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Assay Detail

CHEMBL5529917

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

Binding
Binding affinity to BTK/CRBN (unknown origin) assessed as ternary complex formation measured after 60 mins incubation by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MINO
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein cereblon/Tyrosine-protein kinase BTK (CHEMBL4523704)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases.
Huang J, Ma Z, Peng X, Yang Z, Wu Y, Zhong G, Ouyang T, Chen Z, Liu Y, Wang Q, Chen J, Chen T, Zeng Z.
J Med Chem (2024) 67 : 2438 -2465
PubMed 38321747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.47 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5583871 1 8.56
CHEMBL5583805 1 8.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5583871 EC50 = 2.741 nM 8.56
CHEMBL5583805 EC50 = 4.28 nM 8.37