Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetCoagulation factor X
LigandBDBM18991
Substrate/CompetitorBDBM12500
Meas. Tech.Enzyme Assay and Determination of the Inhibition Constants.
pH7±n/a
Temperature295.15±n/a K
Ki 0.07±n/a nM
Citation Pinto, DJOrwat, MJKoch, SRossi, KAAlexander, RSSmallwood, AWong, PCRendina, ARLuettgen, JMKnabb, RMHe, KXin, BWexler, RRLam, PY 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. J Med Chem50:5339-56 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Coagulation factor X
Name:Coagulation factor X
Synonyms:Activated coagulation factor X (FXa) | Activated factor Xa heavy chain | Coagulation factor X precursor | Coagulation factor Xa | F10 | FA10_HUMAN | 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM18991
BDBM12500
NameBDBM18991
Synonyms:6-[4-(2-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-1-(4-methoxyphenyl)-7-oxo-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridine-3-carboxamide | Pyrazolopyridinone analogue, 13f
TypeSmall organic molecule
Emp. Form.C31H31N5O4
Mol. Mass.537.6089
SMILESCOc1ccc(cc1)-n1nc(C(N)=O)c2CCN(C(=O)c12)c1ccc(cc1)-c1ccccc1CN1CC[C@@H](O)C1 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: