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Assay Detail

CHEMBL2327092

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Binding
Inhibition of chymotrypsin-like activity of proteasome in human NCI-H929 cells after 6 hrs by proteasomeGlo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H929
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proteasome Macropain subunit MB1 (CHEMBL4662)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Incorporation of non-natural amino acids improves cell permeability and potency of specific inhibitors of proteasome trypsin-like sites.
Geurink PP, van der Linden WA, Mirabella AC, Gallastegui N, de Bruin G, Blom AE, Voges MJ, Mock ED, Florea BI, van der Marel GA, Driessen C, van der Stelt M, Groll M, Overkleeft HS, Kisselev AF.
J Med Chem (2013) 56 : 1262 -1275
PubMed 23320547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.21 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326533 1 5.77
CHEMBL2326260 1 5.44
CHEMBL2326261 1 4.98
CHEMBL2326541 1 4.98
CHEMBL2326539 1 4.89
CHEMBL2326272 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326533 IC50 = 1700.0 nM 5.77
CHEMBL2326260 IC50 = 3600.0 nM 5.44
CHEMBL2326261 IC50 = 10500.0 nM 4.98
CHEMBL2326541 IC50 = 10500.0 nM 4.98
CHEMBL2326539 IC50 = 13000.0 nM 4.89
CHEMBL2326272 IC50 > 30000.0 nM -