Assay Detail
Binding
CHEMBL4275380
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of yeast 20S proteasome beta1 subunit using fluorescent substrate pretreated for 30 mins followed by substrate addition and measured after 60 mins by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Saccharomyces cerevisiae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Proteasome subunit beta type-1 (CHEMBL4295578) ↗| Type | SINGLE PROTEIN |
| Organism | Saccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast) |
Publication
Design, synthesis, and evaluation of cystargolide-based β-lactones as potent proteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.45 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4285979 | — | — | 1 | 6.11 |
| CHEMBL4292798 | — | — | 1 | 5.86 |
| CHEMBL4293877 | — | — | 1 | 5.61 |
| CHEMBL4286154 | — | — | 1 | 5.38 |
| CHEMBL4282765 | — | — | 1 | 4.99 |
| CHEMBL4290778 | — | — | 1 | 4.75 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4285979 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL4292798 | — | IC50 | = | 1383.0 | nM | 5.86 |
| CHEMBL4293877 | — | IC50 | = | 2482.0 | nM | 5.61 |
| CHEMBL4286154 | — | IC50 | = | 4178.0 | nM | 5.38 |
| CHEMBL4282765 | — | IC50 | = | 10150.0 | nM | 4.99 |
| CHEMBL4290778 | — | IC50 | = | 17750.0 | nM | 4.75 |
| CHEMBL451887 | CARFILZOMIB | IC50 | > | 1000.0 | nM | - |