Target
Coagulation factor X
Ligand
BDBM50135965
Substrate
n/a
Meas. Tech.
ChEMBL_48828 (CHEMBL661801)
Ki
5.3±n/a nM
Citation
 Pruitt, JRPinto, DJGalemmo, RAAlexander, RSRossi, KAWells, BLDrummond, SBostrom, LLBurdick, DBruckner, RChen, HSmallwood, AWong, PCWright, MRBai, SLuettgen, JMKnabb, RMLam, PYWexler, RR Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1). J Med Chem 46:5298-315 (2003) [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:
BDBM50135965
Synonyms:
2-(4-Methoxy-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | CHEMBL147132
Type:
Small organic molecule
Emp. Form.:
C24H21FN4O4S
Mol. Mass.:
480.511
SMILES:
COc1ccc(cc1)-n1nc(C)cc1C(=O)Nc1ccc(cc1F)-c1ccccc1S(N)(=O)=O
Structure:
Search PDB for entries with ligand similarity: