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Target
Coagulation factor X
Ligand
BDBM12398
Substrate
BDBM12500
Meas. Tech.
Factor Xa Inhibition Assay
pH
7.8±n/a
Temperature
298.15±n/a K
Ki
89±n/a nM
Citation
 Nazare, M; Essrich, M; Will, DW; Matter, H; Ritter, K; Urmann, M; Bauer, A; Schreuder, H; Dudda, A; Czech, J; Lorenz, M; Laux, V; Wehner, V Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents. Bioorg Med Chem Lett 14:4191-5 (2004) [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:
BDBM12398
Synonyms:
1-(3-Methoxy-benzyl)-1H-indole-2-carboxylic acid (1-isopropyl-piperidin-4-yl)-amide | 1-[(3-methoxyphenyl)methyl]-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide | 2-Carboxyindole Scaffold 43 | 2-carboxyindole 12
Type:
Small organic molecule
Emp. Form.:
C25H31N3O2
Mol. Mass.:
405.5325
SMILES:
COc1cccc(Cn2c(cc3ccccc23)C(=O)NC2CCN(CC2)C(C)C)c1
Structure:
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Substrate
Name:
BDBM12500
Synonyms:
Cbz-D-Arg-Gly-L-Arg-pNA | Chromogenic Substrate S-2765 | N-a-Benzyloxycarbonyl-Darginyl-L-glycyl-L-arginine-pnitroaniline | N-alpha-Z-D-Arg-Gly-Arg-p-nitroanilide | benzyl N-[(1R)-4-carbamimidamido-1-[({[(1S)-4-carbamimidamido-1-[(4-nitrophenyl)carbamoyl]butyl]carbamoyl}methyl)carbamoyl]butyl]carbamate
Type:
Small organic molecule
Emp. Form.:
C28H39N11O7
Mol. Mass.:
641.6788
SMILES:
[#7]\[#6](-[#7])=[#7]/[#6]-[#6]-[#6]-[#6@@H](-[#7]-[#6](=O)-[#8]-[#6]-c1ccccc1)-[#6](=O)-[#7]-[#6]-[#6](=O)-[#7]-[#6@@H](-[#6]-[#6]-[#6]-[#7+]=[#6](-[#7])-[#7-])-[#6](=O)-[#7]-c1ccc(cc1)-[#7+](-[#8-])=O |r,w:30.30|
Structure:
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