Assay Detail
Binding
CHEMBL4003672
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Inhibition of chymotrypsin-like activity of human 20S proteasome pretreated for 15 mins followed by Suc-Leu-Leu-Val-Tyr-AMC substrate addition by fluorescence assay
26
Total Activities
26
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
Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.29 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4061262 | — | — | 1 | 9.22 |
| CHEMBL4104744 | — | — | 1 | 9.15 |
| CHEMBL4102324 | — | — | 1 | 9.05 |
| CHEMBL4064404 | — | — | 1 | 9.00 |
| CHEMBL4078056 | — | — | 1 | 9.00 |
| CHEMBL4072652 | — | — | 1 | 8.96 |
| CHEMBL4078693 | — | — | 1 | 8.92 |
| CHEMBL4094582 | — | — | 1 | 8.82 |
| CHEMBL4099839 | — | — | 1 | 8.62 |
| CHEMBL4082676 | — | — | 1 | 8.59 |
| CHEMBL4102973 | — | — | 1 | 8.54 |
| CHEMBL4072186 | — | — | 1 | 8.42 |
| CHEMBL4060792 | — | — | 1 | 8.26 |
| CHEMBL4069929 | — | — | 1 | 8.18 |
| CHEMBL4085936 | — | — | 1 | 8.15 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 8.08 |
| CHEMBL4090916 | — | — | 1 | 8.00 |
| CHEMBL4083128 | — | — | 1 | 7.97 |
| CHEMBL4091814 | — | — | 1 | 7.94 |
| CHEMBL4099146 | — | — | 1 | 7.88 |
| CHEMBL4099557 | — | — | 1 | 7.75 |
| CHEMBL4078258 | — | — | 1 | 7.71 |
| CHEMBL4086778 | — | — | 1 | 7.66 |
| CHEMBL4067120 | — | — | 1 | 7.59 |
| CHEMBL4064053 | — | — | 1 | 7.39 |
| CHEMBL4086868 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4061262 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4104744 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4102324 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4064404 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4078056 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4072652 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4078693 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4094582 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4099839 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4082676 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4102973 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4072186 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4060792 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4069929 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4085936 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4090916 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4083128 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL4091814 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL4099146 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL4099557 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4078258 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL4086778 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL4067120 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL4064053 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4086868 | — | IC50 | = | 192.5 | nM | 6.72 |