Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM13281 |
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Substrate/Competitor | BDBM12593 |
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Meas. Tech. | Enzyme Assay and Determination of the Inhibition Constants. |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 6±n/a nM |
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Citation | Choi-Sledeski, YM; McGarry, DG; Green, DM; Mason, HJ; Becker, MR; Davis, RS; Ewing, WR; Dankulich, WP; Manetta, VE; Morris, RL; Spada, AP; Cheney, DL; Brown, KD; Colussi, DJ; Chu, V; Heran, CL; Morgan, SR; Bentley, RG; Leadley, RJ; Maignan, S; Guilloteau, JP; Dunwiddie, CT; Pauls, HW Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization. J Med Chem42:3572-87 (1999) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, 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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BDBM13281 |
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BDBM12593 |
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Name | BDBM13281 |
Synonyms: | 4-Amino-3-[3-(S)-(7-methoxynaphthalen-2-ylsulfonylamino)-2-oxopyrrolidin-1-ylmethyl]benzamidine | 4-amino-3-{[(3S)-3-[(7-methoxynaphthalene-2-)sulfonamido]-2-oxopyrrolidin-1-yl]methyl}benzene-1-carboximidamide | Sulfonamidopyrrolidinone 4a |
Type | Small organic molecule |
Emp. Form. | C23H25N5O4S |
Mol. Mass. | 467.541 |
SMILES | COc1ccc2ccc(cc2c1)S(=O)(=O)N[C@H]1CCN(Cc2cc(ccc2N)C(N)=N)C1=O |r| |
Structure |
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