Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T84631 | Target Info | |||
| Target Name | Coagulation factor Xa (F10) | ||||
| Synonyms |
Fxa; Factor Xa; F10; Activated coagulation factor X
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| Target Type | Successful Target | ||||
| Gene Name | F10 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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 | Click to Show More | [1] | |
| 2 | Drug Info | Ki = 2.7 nM | [2] | |||
| 3 | BETRIXABAN | Drug Info | IC50 = 18 nM | [3] | ||
| 4 | GW-813893 | Drug Info | Ki = 367 nM | [4] | ||
| 5 | Rivaroxaban | Drug Info | Ki ~ 1000 nM | [6] | ||
| Co-Target Name | Plasminogen (PLG) | Successful Target | ||||
| UniProt ID | PLMN_HUMAN | |||||
| Gene Name | PLG | |||||
| Synonyms |
Plasmin
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| Representative Drug(s) | MELAGATRAN | Drug Info | Ki = 700 nM | [5] | ||
| 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 | [5] | ||
| 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 | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| 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 | Factor Xa inhibitors: next-generation antithrombotic agents. J Med Chem. 2010 Sep 9;53(17):6243-74. | ||||
| REF 3 | Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors. Bioorg Med Chem. 2018 Dec 15;26(23-24):5987-5999. | ||||
| REF 4 | Sulfonamide-related conformational effects and their importance in structure-based design. Bioorg Med Chem Lett. 2007 May 15;17(10):2931-4. | ||||
| REF 5 | Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding. J Med Chem. 2020 Feb 27;63(4):1445-1472. | ||||
| REF 6 | 5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor. J Med Chem. 2013 Dec 12;56(23):9441-56. | ||||
| REF 7 | 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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