Assay Detail
Binding
CHEMBL4433374
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Inhibition of chymotrypsin-like activity of purified human 20S proteasome expressed in human Jurkat cells assessed as decrease in AMC hydrolysis using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 2 hrs by fluorescence based method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Another look at phenolic compounds in cancer therapy the effect of polyphenols on ubiquitin-proteasome system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.18 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 5.82 |
| CHEMBL28 | APIGENIN | — | 1 | 5.75 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 5.46 |
| CHEMBL117 | CHRYSIN | — | 1 | 5.31 |
| CHEMBL164 | MYRICETIN | — | 1 | 5.00 |
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | 4.98 |
| CHEMBL8996 | ERIODICTYOL | — | 1 | 4.79 |
| CHEMBL9352 | NARINGENIN | — | 1 | 4.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL151 | LUTEOLIN | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL28 | APIGENIN | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL50 | QUERCETIN | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL117 | CHRYSIN | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL164 | MYRICETIN | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL150 | KAEMPFEROL | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL8996 | ERIODICTYOL | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL9352 | NARINGENIN | IC50 | = | 48800.0 | nM | 4.31 |