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Target
Coagulation factor X
Ligand
BDBM19023
Substrate
BDBM234442
Meas. Tech.
FXa Inhibition Assay (in prothrombinase)
pH
7.5±0
Temperature
310.15±0 K
Ki
0.72±0.0 nM
Citation
 Luettgen, JM; Knabb, RM; He, K; Pinto, DJ; Rendina, AR Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma. J Enzyme Inhib Med Chem 26:514-26 (2011) [PubMed]  Article 
Target
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:
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEETCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKNCELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERRKRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQECKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGEAVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGIVSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSGGPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPEVITSSPLK
  
Inhibitor
Name:
BDBM19023
Synonyms:
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridine-3-carboxamide | Apixaban | BMS-562247 | CHEMBL231779 | US9938272, Example Apixaban
Type:
Small organic molecule
Emp. Form.:
C25H25N5O4
Mol. Mass.:
459.4971
SMILES:
COc1ccc(cc1)-n1nc(C(N)=O)c2CCN(C(=O)c12)c1ccc(cc1)N1CCCCC1=O
Structure:
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Substrate
Name:
BDBM234442
Synonyms:
N-α-benzyloxycarbonyl-D-Arg-Gly-Arg-pNA | S2765
Type:
Small organic molecule
Emp. Form.:
C28H39N11O7
Mol. Mass.:
641.6788
SMILES:
NC(=N)NCCC[C@H](NC(=O)CNC(=O)[C@@H](CCCNC(N)=N)NC(=O)OCc1ccccc1)C(=O)Nc1ccc(cc1)[N+]([O-])=O |r|
Structure:
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