Therapeutic Targets Database
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TTD Target ID: TTDS00203

Target Information
NameCoagulation factor Xa    
Type of targetSuccessful target    
SynonymsActivated coagulation factor X    
Factor Xa    
Fxa    
DiseaseAtrial fibrillation and flutter
[ICD9: 427.31, 487, 488   ICD10: I48, J10, J11]
[1]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[2][3]
Coagulative disorders
[ICD9: 286   ICD10: D65-D69]
[4][5][6]
Thromboembolic disorders
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[7][8]
Thromboembolism
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[1]
Thrombosis
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[9][10][11]
Thrombotic disease[1][12][3]
Drug(s)Certoparin sodiumApprovedDVT; anticoagulant[13][14][15]
Coagulation Factor IXApprovedChristmas disease (hemophilia B)[16]
DanaparoidApprovedDeep venous clots[17]
EnoxaparinApprovedVenous thromboembolism [18]
Fondaparinux sodiumApprovedVenous thromboembolism [19][20]
Lmw heparinApprovedAnticoagulant[21][22][13]
Nadroparin calciumApprovedAnticoagulant[23][24][13]
RivaroxabanApprovedProphylaxis of deep vein thrombosis in hip and knee replacement surgery
SR-123781APhase III completed, and Positive results in a large European Phase III trialVenous Thromboembolism[25][26]
IdraparinuxPhase III completedThrombosis[27]
AVE5026Phase IIIVTE prevent. in ortho, abdo. surgery, cancer patients[27]
ApixabanPhase IIIAtrial Fibrillation[28][29]
DU-176bPhase IIIAtrial Fibrillation
OtamixabanPhase IICoronary Disease,ACS[27]
PD-348292Phase IIThrombosis[28][30]
TAK-442Phase IIVenous/arterial thromboembolism[31]
GSK813893Phase IPrevention of stroke in patients with atrial fibrillation
OctopamineDiscontinued in Phase IIaThromboembolic Disorders[32][33]
SR-123781ADiscontinued in Phase IIAcute Coronary Syndromes[25][26]
EC NumberEC 3.4.21.6
PathwayComplement and coagulation cascades
UniProt IDP00742
PDB Structure1C5M; 1EZQ; 1F0R; 1F0S; 1FAX; 1FJS; 1FXY; 1G2L; 1G2M; 1HCG; 1IOE; 1IQE; 1IQF; 1IQG; 1IQH; 1IQI; 1IQJ; 1IQK; 1IQL; 1IQM; 1IQN; 1KSN; 1LPG; 1LPK; 1LPZ; 1LQD; 1MQ5; 1MQ6; 1MSX; 1NFU; 1NFW; 1NFX; 1NFY; 1NL8; 1P0S; 1V3X; 1WU1; 1XKA; 1XKB; 1Z6E; 2BMG; 2BOH; 2BOK; 2BQ6; 2BQ7; 2BQW; 2CJI; 2D1J; 2EI6; 2EI7; 2EI8; 2FZZ; 2G00; 2GD4; 2H9E; 2J2U; 2J34; 2J38; 2J4I; 2J94; 2J95; 2JKH; 2P16; 2P3F; 2P3T; 2P3U; 2P93; 2P94; 2P95; 2PHB; 2PR3; 2Q1J; 2RA0; 2UWL; 2UWO; 2UWP; 2VH0; 2VH6; 2VVC; 2VVU; 2VVV; 2VWL; 2VWM; 2VWN; 2VWO; 2W26; 2W3I; 2W3K; 2WYG; 2WYJ; 2XBV; 2XBW; 2XBX; 2XBY; 2XC0; 2XC4; 2XC5; 2Y5F; 2Y5G; 2Y5H; 2Y7X; 2Y7Z; 2Y80; 2Y81; 2Y82; 3CEN; 3CS7; 3ENS; 3FFG; 3HPT; 3IIT; 3K9X; 3KL6; 3KQB; 3KQC; 3KQD; 3KQE; 3LIW; 3M36; 3M37; 3Q3K; 3SW2; 3TK5; 3TK6; 4A7I.    
SequenceMGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE VITSSPLK
Related US Patent6,297,233
6,337,344
6,376,515
6,399,627
6,399,644
6,407,256
6,410,536
6,426,346
6,429,205
6,436,985
6,469,026
6,469,029
6,472,393
6,486,154
6,492,368
6,500,855
6,506,771
6,509,335
6,511,973
6,521,663
6,525,076
6,534,535
6,541,488
6,544,981
6,545,054
6,545,055
6,548,512
6,548,517
6,548,525
6,552,042
6,555,542
6,569,874
6,586,418
6,599,926
6,602,871
6,602,895
6,630,468
6,630,505
6,632,815
6,638,980
6,642,252
6,660,739
6,667,332
6,673,810
6,673,817
6,686,368
6,747,158
Target ValidationClick to Find Target Validation Information.    
InhibitorAVE5026[27]
Antistasin[9]
Apixaban[28][29]
CI-1031[6]
Chloroaniline 1[11]
DPC 423[34]
DX-9065a[12]
DX9065[9]
Danaparoid[17]
Enoxaparin[18]
Fondaparinux[19][20]
Fondaparinux sodium[19][20]
Idraparinux[27]
Lefaxin[9]
M55113[2]
M55551[5]
Octopamine[32][33]
Otamixaban[27]
PD-348292[28][30]
SC-83157[35]
SF303[34]
SK509[34]
SK549[36]
SK554[9]
SN429[35]
SR-123781A[25][26]
T01312[37]
TAK-442[31]
Tick anticoagulant peptide[10][9]
Tick anticoagulant peptide (TAP)[9]
YM-96765[8]
YM60828[9]
ActivatorCoagulation Factor IX[16]
MultitargetSR-123781A[25][26]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Short- and long-acting synthetic pentasaccharides. J Intern Med. 2003 Oct;254(4):335-42. To Reference
Ref 2Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor. Chem Pharm Bull (Tokyo). 2001 Oct;49(10):1237-44. To Reference
Ref 3Novel inhibitors of factor X for use in cardiovascular diseases. Curr Cardiol Rep. 2000 Sep;2(5):395-404. To Reference
Ref 4Determination of the P1', P2' and P3' subsite-specificity of factor Xa. Int J Biochem Cell Biol. 2003 Feb;35(2):221-5. To Reference
Ref 5Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as a factor Xa inhibitor II. Substituent effect on biological activities. Chem Pharm Bull (Tokyo). 2002 Sep;50(9):1187-94. To Reference
Ref 6The antithrombotic effects of CI-1031 (ZK-807834) and enoxaparin in a canine electrolytic injury model of arterial and venous thrombosis. Eur J Pharmacol. 2001 Dec 7;432(2-3):187-94. To Reference
Ref 7Structural basis for chemical inhibition of human blood coagulation factor Xa. Proc Natl Acad Sci U S A. 1998 Jun 9;95(12):6630-5. To Reference
Ref 8Synthesis and biological activity of novel 1,4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity. Bioorg Med Chem. 2004 May 1;12(9):2179-91. To Reference
Ref 9Novel approaches to the treatment of thrombosis. Trends Pharmacol Sci. 2002 Jan;23(1):25-32. To Reference
Ref 10Non-hemostatic activity of coagulation factor Xa: potential implications for various diseases. Curr Opin Pharmacol. 2001 Apr;1(2):169-75. To Reference
Ref 11Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1023-8. To Reference
Ref 12DX-9065a inhibition of factor Xa and the prothrombinase complex: mechanism of inhibition and comparison with therapeutic heparins. Thromb Haemost. 2003 Jan;89(1):112-21. To Reference
Ref 13Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. To Reference
Ref 149684414 To Reference
Ref 1510610007 To Reference
Ref 16Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24. To Reference
Ref 17Effect of factor X inhibition on coagulation activation and cytokine induction in human systemic inflammation. J Infect Dis. 2002 Nov 1;186(9):1270-6. Epub 2002 Oct 8. To Reference
Ref 18In vitro effects of detergent sclerosants on antithrombotic mechanisms. Eur J Vasc Endovasc Surg. 2009 Aug;38(2):220-8. Epub 2009 May 12. To Reference
Ref 19Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24. To Reference
Ref 20Fondaparinux, a synthetic pentasaccharide: the first in a new class of antithrombotic agents - the selective factor Xa inhibitors. Cardiovasc Drug Rev. 2002 Winter;20(1):37-52. To Reference
Ref 21DNP 05 To Reference
Ref 2296 To Reference
Ref 23Prous Integrity database To Reference
Ref 24113585 To Reference
Ref 25SR123781A: a new once-daily synthetic oligosaccharide anticoagulant for thromboprophylaxis after total hip replacement surgery: the DRIVE (Dose Ranging Study in Elective Total Hip Replacement Surgery) study. J Am Coll Cardiol. 2008 Apr 15;51(15):1498-504. To Reference
Ref 26Thromb Haemost. 2001 May;85(5):852-60.SR123781A, a synthetic heparin mimetic. To Reference
Ref 27Pharma & Vaccines. Product Development Pipeline. April 29 2009. To Reference
Ref 28Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 29Pfizer. Report of Pfizer. 0Sep 3 2008. To Reference
Ref 30Pfizer. Report of Pfizer. Oct 14 2008. To Reference
Ref 31Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 32Description of the chemical and pharmacological characteristics of a new hemisynthetic ultra-low-molecular-weight heparin, AVE5026. J Thromb Haemost. 2009 Jul;7(7):1143-51. Epub 2009 Apr 27. To Reference
Ref 33AVE5026, a new hemisynthetic ultra-low-molecular-weight heparin for the prevention of venous thromboembolism in patients after total knee replacement surgery--TREK: a dose-ranging study. J Thromb Haemost. 2009 Apr;7(4):566-72. Epub 2009 Jan 24. To Reference
Ref 34Curr Top Med Chem. 2001 Jun;1(2):137-49.The design and synthesis of noncovalent factor Xa inhibitors. To Reference
Ref 35Pharmacological intervention at disparate sites in the coagulation cascade: comparison of anti-thrombotic efficacy vs bleeding propensity in a rat model of acute arterial thrombosis. J Thromb Thrombolysis. 2002 Oct;14(2):113-21. To Reference
Ref 36Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2. J Med Chem. 1999 Jul 29;42(15):2760-73. To Reference
Ref 37Computer-aided design of a factor Xa inhibitor by using MCSS functionality maps and a CAVEAT linker search. J Mol Graph Model. 2003 Nov;22(2):105-14. To Reference



 

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