Assay Detail
Binding
CHEMBL4123722
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Inhibition of human 20S constitutive proteasome beta-5 using Suc-LLVY-AMC as substrate after 60 mins by fluorescence assay
15
Total Activities
15
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
Potent and Highly Selective Inhibitors of the Proteasome Trypsin-like Site by Incorporation of Basic Side Chain Containing Amino Acid Derived Sulfonyl Fluorides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.05 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129042 | — | — | 1 | 6.68 |
| CHEMBL4128898 | — | — | 1 | 6.02 |
| CHEMBL2326533 | — | — | 1 | 5.58 |
| CHEMBL4125911 | — | — | 1 | 5.17 |
| CHEMBL4128478 | — | — | 1 | 5.05 |
| CHEMBL4129220 | — | — | 1 | 5.00 |
| CHEMBL4126411 | — | — | 1 | 4.75 |
| CHEMBL4129319 | — | — | 1 | 4.56 |
| CHEMBL4126693 | — | — | 1 | 4.41 |
| CHEMBL4130258 | — | — | 1 | 4.17 |
| CHEMBL4127928 | — | — | 1 | 4.16 |
| CHEMBL4128074 | — | — | 1 | - |
| CHEMBL4127967 | — | — | 1 | - |
| CHEMBL4130108 | — | — | 1 | - |
| CHEMBL4129702 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129042 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4128898 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2326533 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4125911 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4128478 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4129220 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4126411 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4129319 | — | IC50 | = | 27800.0 | nM | 4.56 |
| CHEMBL4126693 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4130258 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL4127928 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL4128074 | — | IC50 | = | 140000.0 | nM | - |
| CHEMBL4127967 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4130108 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4129702 | — | IC50 | = | 125000.0 | nM | - |