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Assay Detail

CHEMBL4373370

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

Binding
Stimulation of human 20S proteasome using 11 amino acid FRET peptide as substrate measured every 2 mins over 1 hr by FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

20S proteasome (CHEMBL3831201)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Analysis of chain length, substitution patterns, and unsaturation of AM-404 derivatives as 20S proteasome stimulators.
Coleman RA, Muli CS, Zhao Y, Bhardwaj A, Newhouse TR, Trader DJ.
Bioorg Med Chem Lett (2019) 29 : 420 -423
PubMed 30587447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 4.54 4.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4573271 1 4.62
CHEMBL39878 1 4.55
CHEMBL4561568 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4573271 EC50 = 24000.0 nM 4.62
CHEMBL39878 EC50 = 28000.0 nM 4.55
CHEMBL4561568 EC50 = 35000.0 nM 4.46