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Assay Detail

CHEMBL5508796

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

Binding
Inhibition of USP8 (unknown origin) using Di-Ub IQF K48-02 as substrate preincubated for 30 mins followed by substrate addition by high-throughput assay
2
Total Activities
2
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

Ubiquitin carboxyl-terminal hydrolase 8 (CHEMBL2157854)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364.
Tian Y, Liu K, Wu D, Wu L, Xu Q, Wei W, Li Z, Du Q, Bian J.
Eur J Med Chem (2024) 268 : 116275 -116275
PubMed 38452725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.02 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3392741 1 6.02
CHEMBL5555634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3392741 IC50 = 950.0 nM 6.02
CHEMBL5555634 IC50 < 100.0 nM -