Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM12390 |
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Substrate/Competitor | BDBM12500 |
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Meas. Tech. | Factor Xa Inhibition Assay |
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Ki | 2±n/a nM |
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Citation | Nazare, M; Will, DW; Matter, H; Schreuder, H; Ritter, K; Urmann, M; Essrich, M; Bauer, A; Wagner, M; Czech, J; Lorenz, M; Laux, V; Wehner, V Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography. J Med Chem48:4511-25 (2005) [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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BDBM12390 |
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BDBM12500 |
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Name | BDBM12390 |
Synonyms: | 1-[5-(5-Chlorothiophen-2-yl)isoxazol-3-ylmethyl]-3-fluoro-1H-indole-2-carboxylic Acid (1-Isopropylpiperidin-4-yl)amide | 1-{[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl}-3-fluoro-N-[1-(propan-2-yl)piperidin-4-yl]-1H-indole-2-carboxamide | 2-Carboxyindole Scaffold 22 |
Type | Small organic molecule |
Emp. Form. | C25H26ClFN4O2S |
Mol. Mass. | 501.016 |
SMILES | CC(C)N1CCC(CC1)NC(=O)c1c(F)c2ccccc2n1Cc1cc(on1)-c1ccc(Cl)s1 |
Structure |
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