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Reaction Details
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TargetCoagulation factor X
LigandBDBM17085
Substrate/CompetitorBDBM12658
Meas. Tech.Enzyme Inhibition Assay
pH7.5±n/a
Temperature295.15±n/a K
Ki 1±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 Chem15:2127-46 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Coagulation factor X
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:
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
VITSSPLK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM17085
BDBM12658
NameBDBM17085
Synonyms:3-chloro-N-{4-chloro-2-[(4-chlorophenyl)carbamoyl]phenyl}-4-[(4-methylpiperazin-1-yl)methyl]thiophene-2-carboxamide | Thiophene-Anthranilamide, 2 | thiophene-containing non-amidine inhibitor, 31
TypeSmall organic molecule
Emp. Form.C24H23Cl3N4O2S
Mol. Mass.537.889
SMILESCN1CCN(Cc2csc(C(=O)Nc3ccc(Cl)cc3C(=O)Nc3ccc(Cl)cc3)c2Cl)CC1
Structure
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