Pub. Date : 2019 Dec 15
PMID : 31679971
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | 6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease. | Amiloride | plasminogen activator, urokinase | Rattus norvegicus |
| 2 | In applying the selective optimization of side-activity (SOSA) approach, a focused library of twenty two 6-substituted amiloride derivatives were prepared, with multiple examples displaying uPA inhibitory potencies in the nM range. | Amiloride | plasminogen activator, urokinase | Rattus norvegicus |
| 3 | X-ray co-crystal structures revealed that the potency increases relative to amiloride arise from increased occupancy of uPA"s S1beta subsite by the appended 6-substituents. | Amiloride | plasminogen activator, urokinase | Rattus norvegicus |