Assay Detail
Binding
CHEMBL4255067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 20S constitutive proteasome beta-1 using Z-LLE-betaNA as substrate incubated for 15 mins measured for 45 mins by fluorescence assay
22
Total Activities
22
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
Structure-based design of human immuno- and constitutive proteasomes inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 4.94 | 5.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4287879 | — | — | 1 | 5.67 |
| CHEMBL4279971 | — | — | 1 | 5.66 |
| CHEMBL4282422 | — | — | 1 | 5.58 |
| CHEMBL4281477 | — | — | 1 | 5.57 |
| CHEMBL4278967 | — | — | 1 | 5.33 |
| CHEMBL4289358 | — | — | 1 | 5.31 |
| CHEMBL4294116 | — | — | 1 | 5.22 |
| CHEMBL4285574 | — | — | 1 | 4.94 |
| CHEMBL4290714 | — | — | 1 | 4.91 |
| CHEMBL4292640 | — | — | 1 | 4.89 |
| CHEMBL4290026 | — | — | 1 | 4.87 |
| CHEMBL4286888 | — | — | 1 | 4.82 |
| CHEMBL4290295 | — | — | 1 | 4.77 |
| CHEMBL4293405 | — | — | 1 | 4.76 |
| CHEMBL4277652 | — | — | 1 | 4.75 |
| CHEMBL4280071 | — | — | 1 | 4.70 |
| CHEMBL3237875 | — | — | 1 | 4.66 |
| CHEMBL2337850 | — | — | 1 | 4.52 |
| CHEMBL4290574 | — | — | 1 | 4.50 |
| CHEMBL4290977 | — | — | 1 | 4.46 |
| CHEMBL4280336 | — | — | 1 | 4.40 |
| CHEMBL4288293 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4287879 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL4279971 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4282422 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4281477 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4278967 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4289358 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4294116 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL4285574 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4290714 | — | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL4292640 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4290026 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL4286888 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL4290295 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL4293405 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL4277652 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL4280071 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL3237875 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2337850 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4290574 | — | IC50 | = | 31900.0 | nM | 4.50 |
| CHEMBL4290977 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL4280336 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL4288293 | — | IC50 | = | 46000.0 | nM | 4.34 |