Assay Detail
Binding
CHEMBL2345964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of trypsin-like activity of human constitutive 20s proteasome beta-2 subunit using Boc-LRR-AMC as substrate assessed as remaining activity incubated for 15 mins prior to substrate addition measured after 45 mins by fluorescence assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 12 | 7.01 | 7.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337844 | — | — | 1 | 7.91 |
| CHEMBL2337847 | — | — | 1 | 7.84 |
| CHEMBL2337846 | — | — | 1 | 7.83 |
| CHEMBL2337845 | — | — | 1 | 7.79 |
| CHEMBL2337843 | — | — | 1 | 7.70 |
| CHEMBL2337848 | — | — | 1 | 6.70 |
| CHEMBL2337842 | — | — | 1 | 6.16 |
| CHEMBL2337841 | — | — | 1 | 6.06 |
| CHEMBL2337849 | — | — | 1 | 5.14 |
| CHEMBL2337440 | — | — | 1 | - |
| CHEMBL2337439 | — | — | 1 | - |
| CHEMBL2337850 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337844 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL2337847 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL2337846 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL2337845 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL2337843 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL2337848 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2337842 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2337841 | — | IC50 | = | 867.0 | nM | 6.06 |
| CHEMBL2337849 | — | IC50 | = | 7160.0 | nM | 5.14 |
| CHEMBL2337440 | — | IC50 | - | — | - | |
| CHEMBL2337439 | — | IC50 | - | — | - | |
| CHEMBL2337850 | — | IC50 | - | — | - |