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Assay Detail

CHEMBL3371276

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

Binding
Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proteasome subunit beta type-10 (CHEMBL3317334)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes.
de Bruin G, Huber EM, Xin BT, van Rooden EJ, Al-Ayed K, Kim KB, Kisselev AF, Driessen C, van der Stelt M, van der Marel GA, Groll M, Overkleeft HS.
J Med Chem (2014) 57 : 6197 -6209
PubMed 25006746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.74 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319481 1 6.39
CHEMBL3237875 1 6.23
CHEMBL3319605 1 4.60
CHEMBL3319482 1 -
CHEMBL3319483 1 -
CHEMBL3319577 1 -
CHEMBL3319579 1 -
CHEMBL3319581 1 -
CHEMBL3319591 1 -
CHEMBL3319601 1 -
CHEMBL3319602 1 -
CHEMBL3319603 1 -
CHEMBL3319604 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319481 IC50 = 410.0 nM 6.39
CHEMBL3237875 IC50 = 590.0 nM 6.23
CHEMBL3319605 IC50 = 25000.0 nM 4.60
CHEMBL3319482 IC50 > 10000.0 nM -
CHEMBL3319483 IC50 > 10000.0 nM -
CHEMBL3319577 IC50 > 10000.0 nM -
CHEMBL3319579 IC50 > 10000.0 nM -
CHEMBL3319581 IC50 > 10000.0 nM -
CHEMBL3319591 IC50 > 100000.0 nM -
CHEMBL3319601 IC50 > 100000.0 nM -
CHEMBL3319602 IC50 > 30000.0 nM -
CHEMBL3319603 IC50 > 100000.0 nM -
CHEMBL3319604 IC50 > 100000.0 nM -