Assay Detail
Binding
CHEMBL4394491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of purified human 20S immunoproteasome beta1 subunit using Ac-Pro-Ala-Leu-AMC as substrate pretreated for 1 hr followed by substrate addition and measured at 1 min interval by fluorescence assay
4
Total Activities
4
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
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 | 4 | 6.49 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447840 | — | — | 1 | 7.44 |
| CHEMBL3319605 | — | — | 1 | 6.85 |
| CHEMBL4451741 | — | — | 1 | 6.13 |
| CHEMBL451887 | CARFILZOMIB | 4.0 | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447840 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3319605 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4451741 | — | IC50 | = | 743.5 | nM | 6.13 |
| CHEMBL451887 | CARFILZOMIB | IC50 | = | 2940.0 | nM | 5.53 |