Assay Detail
Binding
CHEMBL4200610
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human kidney uPA using Z-Gly-Gly-Arg-AMC as substrate measured over 15 mins by fluorescence assay
30
Total Activities
30
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 |
Target
Urokinase-type plasminogen activator (CHEMBL3286) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.28 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4211423 | — | — | 1 | 7.68 |
| CHEMBL4208530 | — | — | 1 | 7.39 |
| CHEMBL4215861 | — | — | 1 | 7.38 |
| CHEMBL4206764 | — | — | 1 | 7.38 |
| CHEMBL4204195 | — | — | 1 | 7.37 |
| CHEMBL4217043 | — | — | 1 | 7.28 |
| CHEMBL4207715 | — | — | 1 | 7.06 |
| CHEMBL4212068 | — | — | 1 | 6.97 |
| CHEMBL4208241 | — | — | 1 | 6.81 |
| CHEMBL4216516 | — | — | 1 | 6.78 |
| CHEMBL4213248 | — | — | 1 | 6.74 |
| CHEMBL4203654 | — | — | 1 | 6.64 |
| CHEMBL4216389 | — | — | 1 | 6.50 |
| CHEMBL4203547 | — | — | 1 | 6.29 |
| CHEMBL4210813 | — | — | 1 | 6.18 |
| CHEMBL4211642 | — | — | 1 | 6.05 |
| CHEMBL4218928 | — | — | 1 | 6.03 |
| CHEMBL4203367 | — | — | 1 | 5.99 |
| CHEMBL4207061 | — | — | 1 | 5.88 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | — | 1 | 5.87 |
| CHEMBL4204836 | — | — | 1 | 5.75 |
| CHEMBL4211937 | — | — | 1 | 5.66 |
| CHEMBL4212621 | — | — | 1 | 5.62 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 5.61 |
| CHEMBL4208316 | — | — | 1 | 5.48 |
| CHEMBL4215225 | — | — | 1 | 5.45 |
| CHEMBL4203024 | — | — | 1 | 5.37 |
| CHEMBL4207379 | — | — | 1 | 5.30 |
| CHEMBL4215760 | — | — | 1 | 5.25 |
| CHEMBL4212269 | — | — | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4211423 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4208530 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4215861 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4206764 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4204195 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL4217043 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4207715 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL4212068 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL4208241 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL4216516 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL4213248 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL4203654 | — | Ki | = | 228.0 | nM | 6.64 |
| CHEMBL4216389 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL4203547 | — | Ki | = | 508.0 | nM | 6.29 |
| CHEMBL4210813 | — | Ki | = | 658.0 | nM | 6.18 |
| CHEMBL4211642 | — | Ki | = | 884.0 | nM | 6.05 |
| CHEMBL4218928 | — | Ki | = | 934.0 | nM | 6.03 |
| CHEMBL4203367 | — | Ki | = | 1027.0 | nM | 5.99 |
| CHEMBL4207061 | — | Ki | = | 1319.0 | nM | 5.88 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | Ki | = | 1356.0 | nM | 5.87 |
| CHEMBL4204836 | — | Ki | = | 1778.0 | nM | 5.75 |
| CHEMBL4211937 | — | Ki | = | 2198.0 | nM | 5.66 |
| CHEMBL4212621 | — | Ki | = | 2417.0 | nM | 5.62 |
| CHEMBL945 | AMILORIDE | Ki | = | 2433.0 | nM | 5.61 |
| CHEMBL4208316 | — | Ki | = | 3308.0 | nM | 5.48 |
| CHEMBL4215225 | — | Ki | = | 3539.0 | nM | 5.45 |
| CHEMBL4203024 | — | Ki | = | 4255.0 | nM | 5.37 |
| CHEMBL4207379 | — | Ki | = | 5020.0 | nM | 5.30 |
| CHEMBL4215760 | — | Ki | = | 5670.0 | nM | 5.25 |
| CHEMBL4212269 | — | Ki | = | 16441.0 | nM | 4.78 |