Target
Coagulation factor X
Ligand
BDBM50266890
Substrate
n/a
Meas. Tech.
ChEMBL_563985 (CHEMBL956028)
IC50
0.54±n/a nM
Citation
 Van Huis, CACasimiro-Garcia, ABigge, CFCody, WLDudley, DAFilipski, KJHeemstra, RJKohrt, JTLeadley, RJNarasimhan, LSMcClanahan, TMochalkin, IPamment, MPeterson, JTSahasrabudhe, VSchaum, RPEdmunds, JJ Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action. Bioorg Med Chem 17:2501-11 (2009) [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:
BDBM50266890
Synonyms:
(2R,4R)-N1-(4-Chlorophenyl)-N2-(2-fluoro-4-(3-methyl-2-oxopyridin-1(2H)-yl)phenyl)-4-hydroxy-4-methylpyrrolidine-1,2-dicarboxamide | CHEMBL477228
Type:
Small organic molecule
Emp. Form.:
C25H24ClFN4O4
Mol. Mass.:
498.934
SMILES:
Cc1cccn(-c2ccc(NC(=O)[C@H]3C[C@@](C)(O)CN3C(=O)Nc3ccc(Cl)cc3)c(F)c2)c1=O |r|
Structure:
Search PDB for entries with ligand similarity: