Assay Detail
Binding
CHEMBL4375028
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Inhibition of human 20S proteasome beta 5i preincubated for 1 hr followed by fluorescence based assay
22
Total Activities
22
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 Evaluation of Highly Selective Human Immunoproteasome Inhibitors Reveal a Compensatory Process That Preserves Immune Cell Viability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.96 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4516876 | — | — | 1 | 9.27 |
| CHEMBL4543890 | — | — | 1 | 9.17 |
| CHEMBL4542860 | — | — | 1 | 9.04 |
| CHEMBL4542913 | — | — | 1 | 8.92 |
| CHEMBL4558093 | — | — | 1 | 8.85 |
| CHEMBL4580854 | — | — | 1 | 8.66 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.47 |
| CHEMBL4445016 | — | — | 1 | 8.40 |
| CHEMBL4458214 | — | — | 1 | 8.39 |
| CHEMBL4437785 | — | — | 1 | 8.39 |
| CHEMBL4452844 | — | — | 1 | 8.39 |
| CHEMBL4519222 | — | — | 1 | 8.17 |
| CHEMBL4471761 | — | — | 1 | 8.09 |
| CHEMBL4468132 | — | — | 1 | 7.72 |
| CHEMBL4460338 | — | — | 1 | 7.64 |
| CHEMBL4470266 | — | — | 1 | 7.40 |
| CHEMBL4465040 | — | — | 1 | 7.26 |
| CHEMBL4565027 | — | — | 1 | 7.06 |
| CHEMBL4435165 | — | — | 1 | 6.89 |
| CHEMBL3237875 | — | — | 1 | 6.84 |
| CHEMBL4573625 | — | — | 1 | 6.44 |
| CHEMBL4576544 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4516876 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4543890 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL4542860 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL4542913 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4558093 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4580854 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4445016 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4458214 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4437785 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4452844 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4519222 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4471761 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4468132 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4460338 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4470266 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4465040 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4565027 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4435165 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3237875 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4573625 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4576544 | — | IC50 | = | 2100.0 | nM | 5.68 |