Assay Detail
Binding
CHEMBL4822208
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Inhibition of human chymotrypsin-like beta 5i subunit of iCP using suc-LLVY-AMC as flurogenic substrate for 90 mins by fluorescence-based assay
47
Total Activities
47
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
Discovery of selective fragment-sized immunoproteasome inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 4.55 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854282 | — | — | 1 | 5.75 |
| CHEMBL4871166 | — | — | 1 | 5.52 |
| CHEMBL1724381 | — | — | 1 | 5.39 |
| CHEMBL227686 | — | — | 1 | 5.38 |
| CHEMBL1500876 | — | — | 1 | 5.15 |
| CHEMBL4849565 | — | — | 1 | 5.14 |
| CHEMBL568708 | — | — | 1 | 5.05 |
| CHEMBL4867541 | — | — | 1 | 5.05 |
| CHEMBL4858322 | — | — | 1 | 5.04 |
| CHEMBL4871650 | — | — | 1 | 5.01 |
| CHEMBL4865958 | — | — | 1 | 5.00 |
| CHEMBL4854219 | — | — | 1 | 4.96 |
| CHEMBL4848759 | — | — | 1 | 4.96 |
| CHEMBL4873906 | — | — | 1 | 4.89 |
| CHEMBL111654 | 2-MERCAPTOBENZOTHIAZOLE | — | 1 | 4.89 |
| CHEMBL4877097 | — | — | 1 | 4.82 |
| CHEMBL4858265 | — | — | 1 | 4.80 |
| CHEMBL113414 | — | — | 1 | 4.77 |
| CHEMBL4875943 | — | — | 1 | 4.75 |
| CHEMBL4852689 | — | — | 1 | 4.70 |
| CHEMBL4866283 | — | — | 1 | 4.58 |
| CHEMBL4868002 | — | — | 1 | 4.57 |
| CHEMBL4864399 | — | — | 1 | 4.55 |
| CHEMBL4856216 | — | — | 1 | 4.52 |
| CHEMBL1456330 | — | — | 1 | 4.50 |
| CHEMBL4875672 | — | — | 1 | 4.44 |
| CHEMBL4854026 | — | — | 1 | 4.37 |
| CHEMBL4869230 | — | — | 1 | 4.31 |
| CHEMBL4876125 | — | — | 1 | 4.22 |
| CHEMBL69086 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854282 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4871166 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1724381 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL227686 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1500876 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4849565 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL568708 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4867541 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4858322 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4871650 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4865958 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4854219 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4848759 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4873906 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL111654 | 2-MERCAPTOBENZOTHIAZOLE | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4877097 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4858265 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL113414 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4875943 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4852689 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4866283 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4868002 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4864399 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4856216 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1456330 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4875672 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL4854026 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL4869230 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4876125 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL69086 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL4859482 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL4875334 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL4872203 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL4856015 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL4857254 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL4873052 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL4861417 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL227086 | — | IC50 | = | 94000.0 | nM | 4.03 |
| CHEMBL4867840 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL99703 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL4877930 | — | IC50 | = | 109000.0 | nM | 3.96 |
| CHEMBL70141 | 2-MERCAPTOBENZIMIDAZOLE | IC50 | = | 114000.0 | nM | 3.94 |
| CHEMBL4877640 | — | IC50 | = | 130000.0 | nM | 3.89 |
| CHEMBL4876262 | — | IC50 | = | 129000.0 | nM | 3.89 |
| CHEMBL4868196 | — | IC50 | = | 149000.0 | nM | 3.83 |
| CHEMBL4877725 | — | IC50 | = | 156000.0 | nM | 3.81 |
| CHEMBL1580977 | — | IC50 | - | — | - |