Assay Detail
Binding
CHEMBL4704261
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Inhibition of human constitutive 20S proteasome beta 5 chymotrypsin-like activity
42
Total Activities
42
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
Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 5.57 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784015 | — | — | 1 | 7.26 |
| CHEMBL4759896 | — | — | 1 | 7.23 |
| CHEMBL4764833 | — | — | 1 | 7.00 |
| CHEMBL4764897 | — | — | 1 | 6.92 |
| CHEMBL4747215 | — | — | 1 | 6.77 |
| CHEMBL4758484 | — | — | 1 | 6.61 |
| CHEMBL4751044 | — | — | 1 | 6.53 |
| CHEMBL4754892 | — | — | 1 | 6.52 |
| CHEMBL4746069 | — | — | 1 | 6.51 |
| CHEMBL4784875 | — | — | 1 | 6.37 |
| CHEMBL4782251 | — | — | 1 | 6.29 |
| CHEMBL4796570 | — | — | 1 | 6.21 |
| CHEMBL4798821 | — | — | 1 | 6.01 |
| CHEMBL4763630 | — | — | 1 | 5.98 |
| CHEMBL4758527 | — | — | 1 | 5.88 |
| CHEMBL4741140 | — | — | 1 | 5.84 |
| CHEMBL4764343 | — | — | 1 | 5.83 |
| CHEMBL4779742 | — | — | 1 | 5.59 |
| CHEMBL4776824 | — | — | 1 | 5.46 |
| CHEMBL4763116 | — | — | 1 | 5.26 |
| CHEMBL4782050 | — | — | 1 | 4.97 |
| CHEMBL4762794 | — | — | 1 | 4.89 |
| CHEMBL4764263 | — | — | 1 | 4.88 |
| CHEMBL4799140 | — | — | 1 | 4.86 |
| CHEMBL4744524 | — | — | 1 | 4.84 |
| CHEMBL4784421 | — | — | 1 | 4.73 |
| CHEMBL4776510 | — | — | 1 | 4.68 |
| CHEMBL4745016 | — | — | 1 | 4.64 |
| CHEMBL4754559 | — | — | 1 | 4.57 |
| CHEMBL4516988 | — | — | 1 | 4.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784015 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4759896 | — | IC50 | = | 59.2 | nM | 7.23 |
| CHEMBL4764833 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4764897 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4747215 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4758484 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4751044 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL4754892 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4746069 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL4784875 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL4782251 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL4796570 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4798821 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4763630 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4758527 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4741140 | — | IC50 | = | 1456.0 | nM | 5.84 |
| CHEMBL4764343 | — | IC50 | = | 1467.0 | nM | 5.83 |
| CHEMBL4779742 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL4776824 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL4763116 | — | IC50 | = | 5520.0 | nM | 5.26 |
| CHEMBL4782050 | — | IC50 | = | 10730.0 | nM | 4.97 |
| CHEMBL4762794 | — | IC50 | = | 12730.0 | nM | 4.89 |
| CHEMBL4764263 | — | IC50 | = | 13060.0 | nM | 4.88 |
| CHEMBL4799140 | — | IC50 | = | 13740.0 | nM | 4.86 |
| CHEMBL4744524 | — | IC50 | = | 14340.0 | nM | 4.84 |
| CHEMBL4784421 | — | IC50 | = | 18520.0 | nM | 4.73 |
| CHEMBL4776510 | — | IC50 | = | 20950.0 | nM | 4.68 |
| CHEMBL4745016 | — | IC50 | = | 22730.0 | nM | 4.64 |
| CHEMBL4754559 | — | IC50 | = | 27230.0 | nM | 4.57 |
| CHEMBL4516988 | — | IC50 | = | 32400.0 | nM | 4.49 |
| CHEMBL4745162 | — | IC50 | = | 41080.0 | nM | 4.39 |
| CHEMBL4795707 | — | IC50 | = | 47670.0 | nM | 4.32 |
| CHEMBL4764229 | — | IC50 | = | 53700.0 | nM | 4.27 |
| CHEMBL4741411 | — | IC50 | = | 59030.0 | nM | 4.23 |
| CHEMBL4752685 | — | IC50 | = | 90630.0 | nM | 4.04 |
| CHEMBL4779108 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4753220 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4761864 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4762145 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4754415 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4740404 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4762452 | — | IC50 | > | 100000.0 | nM | - |