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Assay Detail

CHEMBL3371271

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

Binding
Inhibition of proteasome subunit beta-5i in human Raji cells using BODIPY-NC005 by fluorescent densitometry
25
Total Activities
25
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-8 (CHEMBL5620)
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 25 7.89 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319587 1 8.92
CHEMBL3319585 1 8.85
CHEMBL3319478 1 8.70
CHEMBL3319586 1 8.68
CHEMBL3319482 1 8.60
CHEMBL3319578 1 8.52
CHEMBL3319584 1 8.52
CHEMBL3319479 1 8.51
CHEMBL3319588 1 8.48
CHEMBL3319484 1 8.30
CHEMBL3319580 1 8.30
CHEMBL3237875 1 8.24
CHEMBL3319481 1 8.18
CHEMBL3319483 1 8.08
CHEMBL3319579 1 7.96
CHEMBL3319582 1 7.89
CHEMBL3319583 1 7.85
CHEMBL3319581 1 7.50
CHEMBL3319577 1 7.44
CHEMBL3319591 1 7.28
CHEMBL3319480 1 6.61
CHEMBL3319589 1 6.41
CHEMBL3319592 1 6.20
CHEMBL3319590 1 5.24
CHEMBL3319477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319587 IC50 = 1.2 nM 8.92
CHEMBL3319585 IC50 = 1.4 nM 8.85
CHEMBL3319478 IC50 = 2.0 nM 8.70
CHEMBL3319586 IC50 = 2.1 nM 8.68
CHEMBL3319482 IC50 = 2.5 nM 8.60
CHEMBL3319578 IC50 = 3.0 nM 8.52
CHEMBL3319584 IC50 = 3.0 nM 8.52
CHEMBL3319479 IC50 = 3.1 nM 8.51
CHEMBL3319588 IC50 = 3.3 nM 8.48
CHEMBL3319484 IC50 = 5.0 nM 8.30
CHEMBL3319580 IC50 = 5.0 nM 8.30
CHEMBL3237875 IC50 = 5.7 nM 8.24
CHEMBL3319481 IC50 = 6.6 nM 8.18
CHEMBL3319483 IC50 = 8.3 nM 8.08
CHEMBL3319579 IC50 = 11.0 nM 7.96
CHEMBL3319582 IC50 = 13.0 nM 7.89
CHEMBL3319583 IC50 = 14.0 nM 7.85
CHEMBL3319581 IC50 = 32.0 nM 7.50
CHEMBL3319577 IC50 = 36.0 nM 7.44
CHEMBL3319591 IC50 = 53.0 nM 7.28
CHEMBL3319480 IC50 = 244.0 nM 6.61
CHEMBL3319589 IC50 = 392.0 nM 6.41
CHEMBL3319592 IC50 = 632.0 nM 6.20
CHEMBL3319590 IC50 = 5700.0 nM 5.24
CHEMBL3319477 IC50 > 50000.0 nM -