Target Validation Information
TTD ID	T84631
Target Name	Coagulation factor Xa (F10)
Type of Target	Successful
Drug Potency against Target		Drug Info	IC50 = 6250 ng/mL	[16]
	Fondaparinux sodium	Drug Info	IC50 = 130 nM	[15]
	Idraparinux	Drug Info	IC50 = 2.9 nM
	Octopamine	Drug Info	IC50 = 1 nM	[14]
	Otamixaban	Drug Info	Ki = 0.52 nM	[3]
	SR-123781A	Drug Info	IC50 = 77 ng/mL	[13]
	1,2,3,4,6-penta-O-galloyl-beta-D-glucose	Drug Info	Ki = 570 nM	[12]
	4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine	Drug Info	Ki = 1200 nM	[1]
	5-desgalloylstachyurin	Drug Info	Ki = 690 nM	[12]
	BMS-269223	Drug Info	IC50 = 12 nM	[10]
	BMS-344577	Drug Info	Ki = 5.2 nM	[10]
	CASUARIIN	Drug Info	Ki = 450 nM	[12]
	D-Pro-Phe-Arg chloromethyl ketone	Drug Info	IC50 = 1900 nM	[8]
	MELAGATRAN	Drug Info	IC50 = 17300 nM	[4]
	PD-348292	Drug Info	IC50 = 0.57 nM	[9]
	Pedunculagin	Drug Info	Ki = 990 nM	[12]
	PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole)	Drug Info	IC50 = 6 nM	[7]
	RAZAXABAN	Drug Info	Ki = 0.19 nM	[6]
	Rivaroxaban	Drug Info	IC50 = 0.7 nM	[2]
	RWJ-671818	Drug Info	Ki = 3300 nM	[11]
	Tellimagrandin II	Drug Info	Ki = 440 nM	[12]
	ZK-810388	Drug Info	Ki = 0.29 nM	[5]
	ZK-814048	Drug Info	Ki = 2.5 nM	[5]
References
REF 1	Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.
REF 2	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-carb... J Med Chem. 2005 Sep 22;48(19):5900-8.
REF 3	Small molecule coagulation cascade inhibitors in the clinic. Curr Top Med Chem. 2005;5(16):1677-95.
REF 4	Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
REF 5	Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. J Med Chem. 2007 Jun 28;50(13):2967-80.
REF 6	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... J Med Chem. 2007 Nov 1;50(22):5339-56.
REF 7	Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. Bioorg Med Chem. 2008 Feb 15;16(4):1562-95.
REF 8	Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. J Med Chem. 2008 Jun 12;51(11):3077-80.
REF 9	Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action. Bioorg Med Chem. 2009 Mar 15;17(6):2501-11.
REF 10	Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9.
REF 11	Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RW... J Med Chem. 2010 Feb 25;53(4):1843-56.
REF 12	Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. J Nat Prod. 1998 Nov;61(11):1356-60.
REF 13	SR123781A, a synthetic heparin mimetic. Thromb Haemost. 2001 May;85(5):852-60.
REF 14	Targeting the prostaglandin D2 receptors DP and CRTH2 for treatment of inflammation. Curr Top Med Chem. 2006;6(13):1427-44.
REF 15	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.
REF 16	Comparative anticoagulant and platelet modulatory effects of enoxaparin and sulodexide. Clin Appl Thromb Hemost. 2009 Oct;15(5):501-11.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.