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Target
Coagulation factor X
Ligand
BDBM50175078
Substrate
n/a
Meas. Tech.
ChEMBL_326962 (CHEMBL853297)
IC50
10±n/a nM
Citation
 Shi, Y; Zhang, J; Stein, PD; Shi, M; O'Connor, SP; Bisaha, SN; Li, C; Atwal, KS; Bisacchi, GS; Sitkoff, D; Pudzianowski, AT; Liu, EC; Hartl, KS; Seiler, SM; Youssef, S; Steinbacher, TE; Schumacher, WA; Rendina, AR; Bozarth, JM; Peterson, TL; Zhang, G; Zahler, R Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. Bioorg Med Chem Lett 15:5453-8 (2005) [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:
BDBM50175078
Synonyms:
(S,Z)-3-(1-(2-methylbenzofuran-5-ylamino)-3-oxo-3-(thiazol-2-yl)prop-1-enylamino)-1-(2-oxo-2-(pyrrolidin-1-yl)ethyl)azepan-2-one | CHEMBL197542
Type:
Small organic molecule
Emp. Form.:
C27H31N5O4S
Mol. Mass.:
521.631
SMILES:
Cc1cc2cc(ccc2o1)N=C(CC(=O)c1nccs1)N[C@H]1CCCCN(CC(=O)N2CCCC2)C1=O |w:10.11|
Structure:
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