Assay Detail
Binding
CHEMBL4479408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of catalytic activity of constitutive proteasome 20s subunit beta5 in human Raji cells incubated for 1 hr by BODIPY(TMR)-NC-005-VS probe based competitive activity based protein profiling assay
43
Total Activities
36
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Raji |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.65 | 8.70 |
| pIC50(app) | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4534488 | — | — | 2 | 8.70 |
| CHEMBL4581491 | — | — | 2 | 8.68 |
| CHEMBL4563298 | — | — | 2 | 8.68 |
| CHEMBL578478 | — | — | 2 | 8.68 |
| CHEMBL4519899 | — | — | 2 | 8.52 |
| CHEMBL4570216 | — | — | 1 | 8.42 |
| CHEMBL4581001 | — | — | 1 | 8.31 |
| CHEMBL4531811 | — | — | 2 | 7.77 |
| CHEMBL4572766 | — | — | 1 | 7.75 |
| CHEMBL4582677 | — | — | 2 | 7.70 |
| CHEMBL4522536 | — | — | 1 | 7.55 |
| CHEMBL4568033 | — | — | 1 | 7.48 |
| CHEMBL4526232 | — | — | 1 | 7.44 |
| CHEMBL4515448 | — | — | 1 | 7.24 |
| CHEMBL4562527 | — | — | 1 | 7.15 |
| CHEMBL4531320 | — | — | 1 | 6.92 |
| CHEMBL4545125 | — | — | 1 | 6.15 |
| CHEMBL4563143 | — | — | 1 | 6.07 |
| CHEMBL4544082 | — | — | 1 | 6.07 |
| CHEMBL4556581 | — | — | 1 | - |
| CHEMBL4555159 | — | — | 1 | - |
| CHEMBL4588350 | — | — | 1 | - |
| CHEMBL4587878 | — | — | 1 | - |
| CHEMBL4556673 | — | — | 1 | - |
| CHEMBL4574722 | — | — | 1 | - |
| CHEMBL4528476 | — | — | 1 | - |
| CHEMBL4556631 | — | — | 1 | - |
| CHEMBL4522697 | — | — | 1 | - |
| CHEMBL4586866 | — | — | 1 | - |
| CHEMBL3319483 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4534488 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL578478 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4581491 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4563298 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4519899 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4570216 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4581001 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4531811 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4572766 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4582677 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4522536 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4568033 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4526232 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4515448 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4562527 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4531320 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL4545125 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4544082 | — | IC50 | = | 853.0 | nM | 6.07 |
| CHEMBL4563143 | — | IC50 | = | 853.0 | nM | 6.07 |
| CHEMBL4531811 | — | pIC50(app) | = | 7.77 | — | - |
| CHEMBL4581491 | — | pIC50(app) | = | 8.68 | — | - |
| CHEMBL4534488 | — | pIC50(app) | = | 8.7 | — | - |
| CHEMBL4563298 | — | pIC50(app) | = | 8.68 | — | - |
| CHEMBL4519899 | — | pIC50(app) | = | 8.53 | — | - |
| CHEMBL578478 | — | pIC50(app) | = | 8.67 | — | - |
| CHEMBL3319483 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4526408 | — | IC50 | = | 1230000.0 | nM | - |
| CHEMBL4562003 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4586866 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4543267 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4532975 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4560006 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4563141 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4555159 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4582677 | — | pIC50(app) | = | 7.13 | — | - |
| CHEMBL4588350 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4587878 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4556581 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4556673 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4522697 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4556631 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4528476 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4574722 | — | IC50 | < | 10.0 | nM | - |