Target
Coagulation factor X
Ligand
BDBM17236
Substrate
BDBM12658
Meas. Tech.
Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
9.5±n/a nM
Citation
 Kochanny, MJAdler, MEwing, JGriedel, BDHo, EKaranjawala, RLee, WLentz, DLiang, AMMorrissey, MMPhillips, GBPost, JSacchi, KLSakata, STSubramanyam, BVergona, RWalters, JWhite, KAWhitlow, MYe, BZhao, ZShaw, KJ Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa. Bioorg Med Chem 15:2127-46 (2007) [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:
BDBM17236
Synonyms:
2-(4-{[3-chloro-2-({4-chloro-2-[(4-chlorophenyl)carbamoyl]phenyl}carbamoyl)-1-benzothiophen-6-yl]methyl}piperazin-1-yl)acetic acid | benzothiophene compound, 16
Type:
Small organic molecule
Emp. Form.:
C29H25Cl3N4O4S
Mol. Mass.:
631.957
SMILES:
OC(=O)CN1CCN(Cc2ccc3c(Cl)c(sc3c2)C(=O)Nc2ccc(Cl)cc2C(=O)Nc2ccc(Cl)cc2)CC1
Structure:
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Substrate
Name:
BDBM12658
Synonyms:
4-[({[(1S)-4-carbamimidamido-1-[(4-nitrophenyl)carbamoyl]butyl]carbamoyl}methyl)carbamoyl]-4-[(2S,3S)-3-methyl-2-(phenylformamido)pentanamido]butanoic acid hydrochloride | Bz-Ile-Glu-Gly-Arg-pNA | Chromogenic Substrate S-2222 | L-Argininamide, N-benzoyl-L-isoleucyl-L-alpha-glutamylglycyl-N-(4-nitrophenyl)-, monohydrochloride | benzoyl-Ile-Glu-Gly-Arg-p-nitroanilide
Type:
Small organic molecule
Emp. Form.:
C32H43N9O9
Mol. Mass.:
697.7387
SMILES:
[#6]-[#6]-[#6@H](-[#6])-[#6@H](-[#7]-[#6](=O)-c1ccccc1)-[#6](=O)-[#7]-[#6@@H](-[#6]-[#6]-[#6](-[#8])=O)-[#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|
Structure:
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