Assay Detail
Binding
CHEMBL2345514
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Mixed type inhibition of chymotrypsin-like activity of human constitutive 20s proteasome beta-5 subunit using Suc-LLVY-AMC as substrate assessed as inhibition constant for dissociation of enzyme-substrate-inhibitor complex incubated for 15 mins prior to substrate addition measured after 45 mins by fluorescence assay
3
Total Activities
3
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 |
|---|---|---|---|
| Ki | 3 | 6.17 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337842 | — | — | 1 | 6.70 |
| CHEMBL2337841 | — | — | 1 | 6.50 |
| CHEMBL2337849 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337842 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2337841 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL2337849 | — | Ki | = | 5030.0 | nM | 5.30 |