Assay Detail
Binding
CHEMBL4394502
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 20S proteasome beta5 subunit in human RPMI8226 cell lysate using Suc-LLVY-AMC as substrate pretreated for 1 hr followed by substrate addition and measured at 1 min interval by fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.61 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4451741 | — | — | 1 | 8.68 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 8.57 |
| CHEMBL4449204 | — | — | 1 | 8.10 |
| CHEMBL4532449 | — | — | 1 | 6.95 |
| CHEMBL4447840 | — | — | 1 | 5.77 |
| CHEMBL3319605 | — | — | 1 | - |
| CHEMBL4538766 | — | — | 1 | - |
| CHEMBL4529201 | — | — | 1 | - |
| CHEMBL4444547 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4451741 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4449204 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4532449 | — | IC50 | = | 111.6 | nM | 6.95 |
| CHEMBL4447840 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3319605 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4538766 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4529201 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444547 | — | IC50 | > | 1000.0 | nM | - |