Assay Detail
Binding
CHEMBL4682116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S constitutive proteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of PA28alpha incubated for 1 to 2 hrs by fluorescence microplate reader assay
5
Total Activities
5
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
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.15 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787081 | — | — | 1 | 6.36 |
| CHEMBL4749207 | — | — | 1 | 6.17 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 5.92 |
| CHEMBL4749043 | — | — | 1 | - |
| CHEMBL4781914 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787081 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4749207 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4749043 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4781914 | — | IC50 | > | 10000.0 | nM | - |