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Assay Detail

CHEMBL5322833

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Functional
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type TMD8
Confidence 1 — Organism
Curated By Autocuration

Target

TMD8 (CHEMBL4296503)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy.
Chen S, Chen Z, Lu L, Zhao Y, Zhou R, Xie Q, Shu Y, Lin J, Yu X, Wang Y.
Eur J Med Chem (2023) 255 : 115403 -115403
PubMed 37119666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.75 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5403933 1 8.35
CHEMBL1873475 IBRUTINIB 4.0 1 8.33
CHEMBL5438294 1 8.03
CHEMBL5431138 1 7.81
CHEMBL5071105 1 7.34
CHEMBL5413602 1 7.33
CHEMBL5407364 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5403933 IC50 = 4.5 nM 8.35
CHEMBL1873475 IBRUTINIB IC50 = 4.7 nM 8.33
CHEMBL5438294 IC50 = 9.3 nM 8.03
CHEMBL5431138 IC50 = 15.5 nM 7.81
CHEMBL5071105 IC50 = 45.7 nM 7.34
CHEMBL5413602 IC50 = 47.0 nM 7.33
CHEMBL5407364 IC50 = 82.1 nM 7.09