Assay Detail
Binding
CHEMBL981239
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Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit by proteasome active site ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.77 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489864 | — | — | 1 | 8.43 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 8.28 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.06 |
| CHEMBL484004 | — | — | 1 | 8.03 |
| CHEMBL484003 | — | — | 1 | 7.96 |
| CHEMBL483739 | — | — | 1 | 7.85 |
| CHEMBL484156 | — | — | 1 | 7.77 |
| CHEMBL483738 | — | — | 1 | 7.64 |
| CHEMBL483340 | — | — | 1 | 7.44 |
| CHEMBL484002 | — | — | 1 | 7.36 |
| CHEMBL484157 | — | — | 1 | 7.32 |
| CHEMBL483740 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489864 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL484004 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL484003 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL483739 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL484156 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL483738 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL483340 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL484002 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL484157 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL483740 | — | IC50 | = | 73.0 | nM | 7.14 |