Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetCoagulation factor X
LigandBDBM12723
Substrate/CompetitorBDBM12658
Meas. Tech.Enzyme Assay and Determination of the Inhibition Constants.
Ki 2.1±n/a nM
Citation Fevig, JMCacciola, JBuriak, JRossi, KAKnabb, RMLuettgen, JMWong, PCBai, SAWexler, RRLam, PY Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa. Bioorg Med Chem Lett16:3755-60 (2006) [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:
BDBM12723
BDBM12658
NameBDBM12723
Synonyms:6-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-1-(4-methoxyphenyl)-7-oxo-1H,6H,7H-pyrazolo[4,3-d]pyrimidine-3-carbonitrile | pyrazolo[4,3-d]pyrimidinone 40b
TypeSmall organic molecule
Emp. Form.C28H24N6O2
Mol. Mass.476.5292
SMILESCOc1ccc(cc1)-n1nc(C#N)c2ncn(-c3ccc(cc3)-c3ccccc3CN(C)C)c(=O)c12
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: