Assay Detail
Binding
CHEMBL1246539
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Inhibition of PGPH catalytic activity of 20S proteasome beta2 in human LCL cells after 12 hrs
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LCL |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Alpha,beta-unsaturated N-acylpyrrole peptidyl derivatives: new proteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.86 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1240771 | — | — | 1 | 7.44 |
| CHEMBL1240769 | — | — | 1 | 7.21 |
| CHEMBL1243081 | — | — | 1 | 7.19 |
| CHEMBL1243048 | — | — | 1 | 7.04 |
| CHEMBL1240770 | — | — | 1 | 7.01 |
| CHEMBL1243116 | — | — | 1 | 6.91 |
| CHEMBL1240670 | — | — | 1 | 6.81 |
| CHEMBL1243117 | — | — | 1 | 6.75 |
| CHEMBL207990 | EPOXOMYCIN | — | 1 | 5.34 |
| CHEMBL64925 | MG-132 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1240771 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1240769 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1243081 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1243048 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1240770 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1243116 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL1240670 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL1243117 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL207990 | EPOXOMYCIN | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL64925 | MG-132 | IC50 | > | 10000.0 | nM | - |