Assay Detail
Binding
CHEMBL2345965
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of postacid activity of human constitutive 20s proteasome beta-1 subunit using Z-LLE-betaNA 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 | 5.93 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337848 | — | — | 1 | 7.22 |
| CHEMBL2337847 | — | — | 1 | 6.47 |
| CHEMBL2337846 | — | — | 1 | 6.46 |
| CHEMBL2337844 | — | — | 1 | 6.43 |
| CHEMBL2337845 | — | — | 1 | 6.35 |
| CHEMBL2337843 | — | — | 1 | 6.23 |
| CHEMBL2337842 | — | — | 1 | 5.59 |
| CHEMBL2337841 | — | — | 1 | 5.34 |
| CHEMBL2337849 | — | — | 1 | 4.94 |
| CHEMBL2337850 | — | — | 1 | 4.29 |
| CHEMBL2337440 | — | — | 1 | - |
| CHEMBL2337439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337848 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2337847 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL2337846 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL2337844 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2337845 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL2337843 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2337842 | — | IC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL2337841 | — | IC50 | = | 4577.0 | nM | 5.34 |
| CHEMBL2337849 | — | IC50 | = | 11520.0 | nM | 4.94 |
| CHEMBL2337850 | — | IC50 | = | 51200.0 | nM | 4.29 |
| CHEMBL2337440 | — | IC50 | - | — | - | |
| CHEMBL2337439 | — | IC50 | - | — | - |