Assay Detail
Binding
CHEMBL5043595
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Inhibition of human uPA H99Y mutant using pyroGlu-Gly-Arg-pNA as substrate by absorbance based analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 5.16 | 5.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL945 | AMILORIDE | 4.0 | 1 | 5.23 |
| CHEMBL4206764 | — | — | 1 | 5.16 |
| CHEMBL4213248 | — | — | 1 | 5.10 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL945 | AMILORIDE | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL4206764 | — | Ki | = | 6880.0 | nM | 5.16 |
| CHEMBL4213248 | — | Ki | = | 8015.0 | nM | 5.10 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | Ki | > | 50000.0 | nM | - |