Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T89034 | Target Info | |||
Target Name | Plasminogen (PLG) | ||||
Synonyms |
Plasmin
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Target Type | Successful Target | ||||
Gene Name | PLG | ||||
Biochemical Class | Peptidase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Coagulation factor IIa (F2) | Successful Target | ||||
UniProt ID | THRB_HUMAN | |||||
Gene Name | F2 | |||||
Synonyms |
Prothrombin; Coagulation factor II
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Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 1.2 nM | [1] | ||
Co-Target Name | Plasma kallikrein (KLKB1) | Successful Target | ||||
UniProt ID | KLKB1_HUMAN | |||||
Gene Name | KLKB1 | |||||
Synonyms |
Plasma prekallikrein; Plasma kallikrein light chain; Plasma kallikrein heavy chain; PKK; Kininogenin; KLK3; Fletcher factor
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Representative Drug(s) | bis-triazole derivative 10 | Drug Info | Ki = 2.4 nM | [2] | ||
Co-Target Name | Coagulation factor Xa (F10) | Successful Target | ||||
UniProt ID | FA10_HUMAN | |||||
Gene Name | F10 | |||||
Synonyms |
Fxa; Factor Xa; F10; Activated coagulation factor X
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Representative Drug(s) | bis-triazole derivative 10 | Drug Info | Ki = 206 nM | [2] | ||
Co-Target Name | Tissue-type plasminogen activator (PLAT) | Successful Target | ||||
UniProt ID | TPA_HUMAN | |||||
Gene Name | PLAT | |||||
Synonyms |
TPA; T-plasminogen activator; T-PA; Reteplase; Alteplase
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Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 900 nM | [3] | ||
Co-Target Name | Trypsin (TRY) | Co-Target | ||||
UniProt ID | TRY1_HUMAN; TRY2_HUMAN; TRY3_HUMAN | |||||
Gene Name | PRSS1; PRSS2; PRSS3 | |||||
Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 4.3 nM | [4] |
References | Top | ||||
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REF 1 | Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1017-22. | ||||
REF 2 | A new strategy for the development of highly potent and selective plasmin inhibitors. J Med Chem. 2012 Feb 9;55(3):1171-80. | ||||
REF 3 | Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding. J Med Chem. 2020 Feb 27;63(4):1445-1472. | ||||
REF 4 | Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4779-84. |
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