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TargetCoagulation factor X
LigandBDBM12681
Substrate/CompetitorBDBM12658
Meas. Tech.Enzyme Assay and Determination of the Inhibition Constants.
pH7±n/a
Temperature295.15±n/a K
Ki 0.04±n/a nM
Citation Pinto DJGalemmo RAQuan MLOrwat MJClark CLi RWells BWoerner FAlexander RSRossi KASmallwood AWong PCLuettgen JMRendina ARKnabb RMHe KWexler RRLam PY Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties. Bioorg Med Chem Lett 16:5584-9 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Coagulation factor X
Name:Thrombin and coagulation factor X
Synonyms:Activated coagulation factor X (FXa) | Activated factor Xa heavy chain | Coagulation factor X precursor | Coagulation factor Xa | F10 | Factor X heavy chain | Factor X light chain | Factor Xa | Stuart factor | Stuart-Prower factor
Type:Enzyme
Mol. Mass.:54726.60
Organism:Homo sapiens (Human)
Description:n/a
Residue:488
Sequence:
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
VITSSPLK
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  Blast E-value cutoff:
BDBM12681
BDBM12658
NameBDBM12681
Synonyms:1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one | BMS-740808 Analogue 6a | bicyclic pyrazole scaffold | dihydropyrazolopyridinone analogue 9
TypeSmall organic molecule
Emp. Form.C29H25F3N6O2
Mol. Mass.546.543
SMILESCN(C)Cc1ccccc1-c1ccc(cc1)N1CCc2c(nn(c2C1=O)-c1ccc2onc(N)c2c1)C(F)(F)F
Structure
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