Assay Detail
Binding
CHEMBL3128372
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 20s constitutive proteasome beta 2 subunit trypsin-like activity in rabbit erythrocytes using Boc-LRR-AMC as substrate incubated for 15 mins prior to substrate addition measured after 45 mins by fluorescence assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
New C(4)- and C(1)-derivatives of furo[3,4-c]pyridine-3-ones and related compounds: evidence for site-specific inhibition of the constitutive proteasome and its immunoisoform.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 4.84 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371405 | MARIZOMIB | 3.0 | 1 | 7.68 |
| CHEMBL3128155 | — | — | 1 | 5.06 |
| CHEMBL3128248 | — | — | 1 | 5.00 |
| CHEMBL3128249 | — | — | 1 | 4.71 |
| CHEMBL3128149 | — | — | 1 | 4.32 |
| CHEMBL3128167 | — | — | 1 | 4.25 |
| CHEMBL3128156 | — | — | 1 | 4.23 |
| CHEMBL3128147 | — | — | 1 | 4.22 |
| CHEMBL3128257 | — | — | 1 | 4.06 |
| CHEMBL3128148 | — | — | 1 | - |
| CHEMBL3128150 | — | — | 1 | - |
| CHEMBL3128151 | — | — | 1 | - |
| CHEMBL3128152 | — | — | 1 | - |
| CHEMBL3128153 | — | — | 1 | - |
| CHEMBL3128154 | — | — | 1 | - |
| CHEMBL3128157 | — | — | 1 | - |
| CHEMBL3128158 | — | — | 1 | - |
| CHEMBL3128159 | — | — | 1 | - |
| CHEMBL3128161 | — | — | 1 | - |
| CHEMBL3128254 | — | — | 1 | - |
| CHEMBL3128146 | — | — | 1 | - |
| CHEMBL3128145 | — | — | 1 | - |
| CHEMBL3128144 | — | — | 1 | - |
| CHEMBL3128143 | — | — | 1 | - |
| CHEMBL3128140 | — | — | 1 | - |
| CHEMBL3128255 | — | — | 1 | - |
| CHEMBL3128256 | — | — | 1 | - |
| CHEMBL3128253 | — | — | 1 | - |
| CHEMBL3128260 | — | — | 1 | - |
| CHEMBL3128258 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371405 | MARIZOMIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3128155 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3128248 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL3128249 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL3128149 | — | IC50 | = | 48100.0 | nM | 4.32 |
| CHEMBL3128167 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL3128156 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL3128147 | — | IC50 | = | 60800.0 | nM | 4.22 |
| CHEMBL3128257 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL3128150 | — | IC50 | - | — | - | |
| CHEMBL3124973 | — | IC50 | - | — | - | |
| CHEMBL3128151 | — | IC50 | - | — | - | |
| CHEMBL3128152 | — | IC50 | - | — | - | |
| CHEMBL3128153 | — | IC50 | - | — | - | |
| CHEMBL3128154 | — | IC50 | - | — | - | |
| CHEMBL3128157 | — | IC50 | - | — | - | |
| CHEMBL3128158 | — | IC50 | - | — | - | |
| CHEMBL3128159 | — | IC50 | - | — | - | |
| CHEMBL3128161 | — | IC50 | - | — | - | |
| CHEMBL3128164 | — | IC50 | - | — | - | |
| CHEMBL3128165 | — | IC50 | - | — | - | |
| CHEMBL3128148 | — | IC50 | - | — | - | |
| CHEMBL3128254 | — | IC50 | - | — | - | |
| CHEMBL3128146 | — | IC50 | - | — | - | |
| CHEMBL3128145 | — | IC50 | - | — | - | |
| CHEMBL3128144 | — | IC50 | - | — | - | |
| CHEMBL3128143 | — | IC50 | - | — | - | |
| CHEMBL3128140 | — | IC50 | - | — | - | |
| CHEMBL3128255 | — | IC50 | - | — | - | |
| CHEMBL3128256 | — | IC50 | - | — | - | |
| CHEMBL3128253 | — | IC50 | - | — | - | |
| CHEMBL3128260 | — | IC50 | - | — | - | |
| CHEMBL3128258 | — | IC50 | - | — | - |