| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T84631 | ||||
| Target Name | Coagulation factor Xa | ||||
| Target Type | Investigate |
||||
| Drug Potency against Target | Idraparinux | Drug Info | IC50 = 2.9 nM | ||
| PEDUNCULAGIN | Drug Info | Ki = 990 nM | [534762] | ||
| PD-348292 | Drug Info | IC50 = 0.57 nM | [529972] | ||
| Rivaroxaban | Drug Info | IC50 = 0.7 nM | [527736] | ||
| 1,2,3,4,6-penta-O-galloyl-beta-D-glucose | Drug Info | Ki = 570 nM | [534762] | ||
| CASUARIIN | Drug Info | Ki = 450 nM | [534762] | ||
| RWJ-671818 | Drug Info | Ki = 3300 nM | [530660] | ||
| MELAGATRAN | Drug Info | IC50 = 17300 nM | [528066] | ||
| ZK-814048 | Drug Info | Ki = 2.5 nM | [528872] | ||
| Fondaparinux sodium | Drug Info | IC50 = 130 nM | [552832] | ||
| 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine | Drug Info | Ki = 1200 nM | [527397] | ||
| SR-123781A | Drug Info | IC50 = 77 ng/mL | [535183] | ||
| D-Pro-Phe-Arg chloromethyl ketone | Drug Info | IC50 = 1900 nM | [529454] | ||
| PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole) | Drug Info | IC50 = 6 nM | [529193] | ||
| ZK-810388 | Drug Info | Ki = 0.29 nM | [528872] | ||
| BMS-269223 | Drug Info | IC50 = 12 nM | [530503] | ||
| Enoxaparin | Drug Info | IC50 = 6250 ng/mL | [552976] | ||
| RAZAXABAN | Drug Info | Ki = 0.19 nM | [529078] | ||
| BMS-344577 | Drug Info | Ki = 5.2 nM | [530503] | ||
| Tellimagrandin II | Drug Info | Ki = 440 nM | [534762] | ||
| 5-desgalloylstachyurin | Drug Info | Ki = 690 nM | [534762] | ||
| Octopamine | Drug Info | IC50 = 1 nM | [552628] | ||
| Otamixaban | Drug Info | Ki = 0.52 nM | [527940] | ||
| References | |||||
| Ref 534762 | J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. | ||||
| Ref 529972 | Bioorg Med Chem. 2009 Mar 15;17(6):2501-11. Epub 2009 Feb 3.Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action. | ||||
| Ref 527736 | J Med Chem. 2005 Sep 22;48(19):5900-8.Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor. | ||||
| Ref 534762 | J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. | ||||
| Ref 534762 | J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. | ||||
| Ref 530660 | J Med Chem. 2010 Feb 25;53(4):1843-56.Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif. | ||||
| Ref 528066 | Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. | ||||
| Ref 528872 | J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. | ||||
| Ref 552832 | Monitoring direct FXa-inhibitors and fondaparinux by Prothrombinase-induced Clotting Time (PiCT): relation to FXa-activity and influence of assay modifications. Thromb Res. 2008;123(2):396-403. doi: 10.1016/j.thromres.2008.05.010. Epub 2008 Jun 24. | ||||
| Ref 527397 | Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. | ||||
| Ref 535183 | SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60. | ||||
| Ref 529454 | J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. | ||||
| Ref 529193 | Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. Epub 2007 Nov 6.Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. | ||||
| Ref 528872 | J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. | ||||
| Ref 530503 | Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. | ||||
| Ref 552976 | Comparative anticoagulant and platelet modulatory effects of enoxaparin and sulodexide. Clin Appl Thromb Hemost. 2009 Oct;15(5):501-11. doi: 10.1177/1076029609338711. Epub 2009 Aug 23. | ||||
| Ref 529078 | J Med Chem. 2007 Nov 1;50(22):5339-56. Epub 2007 Oct 3.Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban,BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. | ||||
| Ref 530503 | Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. | ||||
| Ref 534762 | J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. | ||||
| Ref 534762 | J Nat Prod. 1998 Nov;61(11):1356-60.Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. | ||||
| Ref 552628 | Targeting the prostaglandin D2 receptors DP and CRTH2 for treatment of inflammation. Curr Top Med Chem. 2006;6(13):1427-44. | ||||
| Ref 527940 | Curr Top Med Chem. 2005;5(16):1677-95.Small molecule coagulation cascade inhibitors in the clinic. | ||||
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