Assay Detail
Binding
CHEMBL4375035
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Inhibition of 20S proteasome beta 5i/20S proteasome beta 1i in human PBMC cell lysate assessed as reduction in chymotrypsin-like activity pre-incubated for 30 mins followed by Meo-Suc-GLF-AM substrate addition and measured after 30 mins by fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Lysate |
| 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 | 18 | 7.15 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4516876 | — | — | 1 | 8.64 |
| CHEMBL4542860 | — | — | 1 | 8.49 |
| CHEMBL4543890 | — | — | 1 | 8.16 |
| CHEMBL4542913 | — | — | 1 | 7.96 |
| CHEMBL4558093 | — | — | 1 | 7.60 |
| CHEMBL4580854 | — | — | 1 | 7.47 |
| CHEMBL4445016 | — | — | 1 | 7.35 |
| CHEMBL4437785 | — | — | 1 | 7.22 |
| CHEMBL4452844 | — | — | 1 | 7.10 |
| CHEMBL4458214 | — | — | 1 | 7.10 |
| CHEMBL4460338 | — | — | 1 | 7.07 |
| CHEMBL4519222 | — | — | 1 | 6.89 |
| CHEMBL4468132 | — | — | 1 | 6.70 |
| CHEMBL4465040 | — | — | 1 | 6.60 |
| CHEMBL4470266 | — | — | 1 | 6.54 |
| CHEMBL4435165 | — | — | 1 | 6.51 |
| CHEMBL4565027 | — | — | 1 | 6.33 |
| CHEMBL4573625 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4516876 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4542860 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4543890 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4542913 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4558093 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4580854 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4445016 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4437785 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4452844 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4458214 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4460338 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4519222 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4468132 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4465040 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4470266 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4435165 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4565027 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4573625 | — | IC50 | = | 8900.0 | nM | 5.05 |