Therapeutic Targets Database
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TTD Target ID: TTDR00151

Target Information
NameCoagulation factor X    
Type of targetResearch target    
SynonymsFactor X    
Stuart factor    
Stuart-Prower factor    
DiseaseThrombosis
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[1][2]
Thrombotic disease[3]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.21.6
PathwayComplement and coagulation cascades
UniProt IDP00742
PDB Structure1C5M; 1EZQ; 1F0R; 1F0S; 1FAX; 1FJS; 1FXY; 1G2L.    
FunctionFactor xa is a vitamin k-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor va, calcium and phospholipid during blood clotting.    
SequenceMGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE VITSSPLK
Target ValidationClick to Find Target Validation Information.    
Inhibitor3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate[4]
4- (4-Benzyloxy-3-methoxy-benzylamino)-benzamidine[5]
5-desgalloylstachyurin[6]
Azaphenylalanine derivative[7]
Azaphenylalanine derivative[7]
Azaphenylalanine derivative[7]
Azaphenylalanine derivative[7]
BAY-59-7939[8]
BMS-269223[9]
BMS-344577[9]
BMS-740808[10]
Beta-Hydroxy Aspartic Acid[11]
CASUARIIN[6]
D-Pro-Phe-Arg chloromethyl ketone[12]
ERIBAXABAN[13]
Gamma-Carboxy-Glutamic Acid[14]
MELAGATRAN[15]
PEDUNCULAGIN[6]
PhSO2-Gly- (Me-Gly)-Arg-[16]
RAZAXABAN[10]
RAZAXABAN HYDROCHLORIDE[17]
RWJ-671818[18]
SN-429[19]
Tissue factor pathway inhibitor (TFPI)[3]
ZK-810388[20]
ZK-813039[20]
ZK-814048[20]
penta-O-galloyl-beta-glucoside[6]
tellimagrandin II[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Novel inhibitors of factor X for use in cardiovascular diseases. Curr Cardiol Rep. 2000 Sep;2(5):395-404. To Reference
Ref 2Moving Up the Coagulation Cascade: Potential Factor X Inhibition for Percutaneous Coronary Intervention. Curr Interv Cardiol Rep. 2001 Aug;3(3):251-259. To Reference
Ref 3Role of tissue factor pathway inhibitor in the regulation of tissue factor-dependent blood coagulation. Cardiovasc Drug Rev. 2002 Winter;20(1):67-80. To Reference
Ref 4J Med Chem. 2005 Dec 1;48(24):7592-603.3,6-disubstituted coumarins as mechanism-based inhibitors of thrombin and factor Xa. To Reference
Ref 5Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. To Reference
Ref 6J 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. To Reference
Ref 7Bioorg Med Chem Lett. 2004 Mar 22;14(6):1563-7.Thrombin inhibitors built on an azaphenylalanine scaffold. To Reference
Ref 8J 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. To Reference
Ref 9Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. To Reference
Ref 10J 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. To Reference
Ref 11Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 12J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. To Reference
Ref 13Bioorg 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. To Reference
Ref 14Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 15Bioorg 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. To Reference
Ref 16Bioorg 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. To Reference
Ref 17Bioorg Med Chem Lett. 2006 Oct 1;16(19):5176-82. Epub 2006 Jul 25.Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa. To Reference
Ref 18J 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. To Reference
Ref 19Bioorg Med Chem Lett. 2004 Nov 1;14(21):5263-7.SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa. To Reference
Ref 20J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. To Reference



 

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