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Assay Detail

CHEMBL868170

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

Binding
Inhibition of chymotrypsin like activity of yeast 20S proteasome
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Saccharomyces cerevisiae
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Proteasome Macropain subunit PRE2 (CHEMBL4659)
Type SINGLE PROTEIN
Organism Saccharomyces cerevisiae S288c

Publication

Development of lipopeptides for inhibiting 20S proteasomes.
Basse N, Papapostolou D, Pagano M, Reboud-Ravaux M, Bernard E, Felten AS, Vanderesse R.
Bioorg Med Chem Lett (2006) 16 : 3277 -3281
PubMed 16630721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 4.48 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210325 1 5.30
CHEMBL100097 1 4.75
CHEMBL209568 1 4.70
CHEMBL210871 1 4.70
CHEMBL208689 1 4.70
CHEMBL439509 1 4.55
CHEMBL380390 1 4.52
CHEMBL209984 1 4.52
CHEMBL425955 1 4.47
CHEMBL377322 1 4.43
CHEMBL279186 1 4.41
CHEMBL379309 1 4.37
CHEMBL379749 1 4.37
CHEMBL378000 1 4.14
CHEMBL207660 1 4.10
CHEMBL267439 1 4.10
CHEMBL207452 1 4.09
CHEMBL378865 1 -
CHEMBL425052 1 -
CHEMBL209258 1 -
CHEMBL378045 1 -
CHEMBL426136 1 -
CHEMBL209290 1 -
CHEMBL379316 1 -
CHEMBL277277 1 -
CHEMBL378002 1 -
CHEMBL426505 1 -
CHEMBL210501 1 -
CHEMBL380055 1 -
CHEMBL378655 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210325 Ki = 5000.0 nM 5.30
CHEMBL100097 Ki = 18000.0 nM 4.75
CHEMBL209568 Ki = 20000.0 nM 4.70
CHEMBL210871 Ki = 20000.0 nM 4.70
CHEMBL208689 Ki = 20000.0 nM 4.70
CHEMBL439509 Ki = 28000.0 nM 4.55
CHEMBL380390 Ki = 30000.0 nM 4.52
CHEMBL209984 Ki = 30000.0 nM 4.52
CHEMBL425955 Ki = 34000.0 nM 4.47
CHEMBL377322 Ki = 37000.0 nM 4.43
CHEMBL279186 Ki = 39000.0 nM 4.41
CHEMBL379309 Ki = 43000.0 nM 4.37
CHEMBL379749 Ki = 43000.0 nM 4.37
CHEMBL378000 Ki = 72000.0 nM 4.14
CHEMBL207660 Ki = 80000.0 nM 4.10
CHEMBL267439 Ki = 80000.0 nM 4.10
CHEMBL207452 Ki = 81000.0 nM 4.09
CHEMBL378865 Ki > 80000.0 nM -
CHEMBL425052 Ki > 80000.0 nM -
CHEMBL209258 Ki > 80000.0 nM -
CHEMBL378045 Ki = 619000.0 nM -
CHEMBL426136 Ki > 625000.0 nM -
CHEMBL209290 Ki > 80000.0 nM -
CHEMBL379316 Ki > 80000.0 nM -
CHEMBL277277 Ki = 151000.0 nM -
CHEMBL378002 Ki > 625000.0 nM -
CHEMBL426505 Ki > 625000.0 nM -
CHEMBL210501 Ki = 545000.0 nM -
CHEMBL380055 Ki > 625000.0 nM -
CHEMBL378655 Ki = 139000.0 nM -