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Assay Detail

CHEMBL615353

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

Binding
Compound was evaluated for inhibitory activity against 20S proteasome from human liver and brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent inhibitors of proteasome.
Iqbal M, Chatterjee S, Kauer JC, Das M, Messina P, Freed B, Biazzo W, Siman R.
J Med Chem (1995) 38 : 2276 -2277
PubMed 7608891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307387 1 8.70
CHEMBL74336 1 8.22
CHEMBL2114122 1 7.70
CHEMBL76284 1 7.40
CHEMBL73602 1 7.02
CHEMBL2369773 1 6.00
CHEMBL406736 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307387 IC50 = 2.0 nM 8.70
CHEMBL74336 IC50 = 6.0 nM 8.22
CHEMBL2114122 IC50 = 20.0 nM 7.70
CHEMBL76284 IC50 = 40.0 nM 7.40
CHEMBL73602 IC50 = 95.0 nM 7.02
CHEMBL2369773 IC50 = 1000.0 nM 6.00
CHEMBL406736 IC50 > 3000.0 nM -