Reaction Details |
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Target | Coagulation factor X |
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Ligand | BDBM50242831 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_491893 (CHEMBL946423) |
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Ki | 0.14±n/a nM |
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Citation | Qiao, JX; Cheney, DL; Alexander, RS; Smallwood, AM; King, SR; He, K; Rendina, AR; Luettgen, JM; Knabb, RM; Wexler, RR; Lam, PY Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa. Bioorg Med Chem Lett18:4118-23 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50242831 |
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n/a |
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Name | BDBM50242831 |
Synonyms: | 3-ethyl-1-((1-(4-(1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazolo[3,4-c]pyridin-6(7H)-yl)phenyl)cyclopropyl)methyl)-1-methylurea | CHEMBL517711 |
Type | Small organic molecule |
Emp. Form. | C28H30F3N5O3 |
Mol. Mass. | 541.5647 |
SMILES | CCNC(=O)N(C)CC1(CC1)c1ccc(cc1)N1CCc2c(nn(c2C1=O)-c1ccc(OC)cc1)C(F)(F)F |
Structure |
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