Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM15848 |
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Substrate/Competitor | BDBM12500 |
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Meas. Tech. | Factor Xa Inhibition Assay |
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Ki | 12±n/a nM |
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Citation | Nazare, M; Essrich, M; Will, DW; Matter, H; Ritter, K; Urmann, M; Bauer, A; Schreuder, H; Czech, J; Lorenz, M; Laux, V; Wehner, V Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand. Bioorg Med Chem Lett14:4197-201 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Coagulation factor X |
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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
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BDBM15848 |
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BDBM12500 |
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Name | BDBM15848 |
Synonyms: | 1-{[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl}-N-[1-(pyridin-4-yl)azetidin-3-yl]-1H-indole-2-carboxamide | 2-carboxyindole-based inhibitor 33 |
Type | Small organic molecule |
Emp. Form. | C25H20ClN5O2S |
Mol. Mass. | 489.977 |
SMILES | Clc1ccc(s1)-c1cc(Cn2c(cc3ccccc23)C(=O)NC2CN(C2)c2ccncc2)no1 |
Structure |
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