Assay Detail
Binding
CHEMBL2345512
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Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.55 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL64925 | MG-132 | — | 1 | 8.05 |
| CHEMBL207990 | EPOXOMYCIN | — | 1 | 7.58 |
| CHEMBL2337841 | — | — | 1 | 6.60 |
| CHEMBL2337845 | — | — | 1 | 6.33 |
| CHEMBL2337846 | — | — | 1 | 6.32 |
| CHEMBL2337843 | — | — | 1 | 6.27 |
| CHEMBL2337844 | — | — | 1 | 6.12 |
| CHEMBL2337849 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL64925 | MG-132 | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL207990 | EPOXOMYCIN | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2337841 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL2337845 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL2337846 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL2337843 | — | IC50 | = | 541.0 | nM | 6.27 |
| CHEMBL2337844 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL2337849 | — | IC50 | = | 7970.0 | nM | 5.10 |