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Assay Detail

CHEMBL1112366

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

Binding
Inhibition of chymotrypsin like activity of yeast 20S proteasome beta 5 subunit after 30 mins by fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Saccharomyces cerevisiae
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Function-oriented biosynthesis of beta-lactone proteasome inhibitors in Salinispora tropica.
Nett M, Gulder TA, Kale AJ, Hughes CC, Moore BS.
J Med Chem (2009) 52 : 6163 -6167
PubMed 19746976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.39 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371405 MARIZOMIB 3.0 1 8.72
CHEMBL1077383 SALINOSPORAMIDE X7 1 8.66
CHEMBL1081673 1 8.03
CHEMBL192046 1 7.56
CHEMBL1081854 SALINOSPORAMIDE X3 1 7.03
CHEMBL561240 ANTIPROTEALIDE 1 7.00
CHEMBL1080762 SALINOSPORAMIDE X6 1 6.88
CHEMBL1077389 SALINOSPORAMIDE X5 1 6.61
CHEMBL1080230 SALINOSPORAMIDE X4 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371405 MARIZOMIB IC50 = 1.9 nM 8.72
CHEMBL1077383 SALINOSPORAMIDE X7 IC50 = 2.2 nM 8.66
CHEMBL1081673 IC50 = 9.3 nM 8.03
CHEMBL192046 IC50 = 27.5 nM 7.56
CHEMBL1081854 SALINOSPORAMIDE X3 IC50 = 93.4 nM 7.03
CHEMBL561240 ANTIPROTEALIDE IC50 = 101.0 nM 7.00
CHEMBL1080762 SALINOSPORAMIDE X6 IC50 = 132.0 nM 6.88
CHEMBL1077389 SALINOSPORAMIDE X5 IC50 = 245.0 nM 6.61
CHEMBL1080230 SALINOSPORAMIDE X4 IC50 = 1029.0 nM 5.99