Ki Summary

Reaction Details

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Target

Coagulation factor X

Ligand

BDBM50324743

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_651366 (CHEMBL1227186)

100±n/a nM

Citation

Anselm, L; Banner, DW; Benz, J; Zbinden, KG; Himber, J; Hilpert, H; Huber, W; Kuhn, B; Mary, JL; Otteneder, MB; Panday, N; Ricklin, F; Stahl, M; Thomi, S; Haap, W Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate. Bioorg Med Chem Lett20:5313-9 (2010) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Coagulation factor X

Name:

Coagulation factor X

Synonyms:

Coagulation factor X precursor | F10 | FA10_RAT | Factor Xa (fXa) | Stuart factor

Type:

Enzyme

Mol. Mass.:

54255.03

Organism:

Rattus norvegicus (rat)

Description:

n/a

Residue:

482

Sequence:

MESPVRLSLLYVVLASLLLPGRSVFINRERANNVLQRIRRANSFFEEIKKGNLERECVEE
ICSFEEAREVFEDNEKTTEFWNKYEDGDQCESSPCQNQGECRDGLGSYTCTCTEGFEGKN
CELFVRKLCSLDNGDCDQFCREEQNSVVCSCAKGYFLGNDGKSCLSTAPFPCGKTNKGRA
KRSVALNTSNSEPDPEDLMPDADILYPTESPSELLNLNKTEPEANSDDVIRIVGGQECKR
GECPWQALLFSDEETDGFCGGTILNEFYILTAAHCLHQAKRFKVRVGDLNTEQEDGGEMV
HEVDMIIKHNKFQRDTYDFDIAMLRLKTPITFRENVAPACLPQKDWAEATLMTQKTGIVS
GFGRTHEKGRQSKVLKMMEVPYVDRNTCRLSTSFSITQNMFCAGYDAKQEDACQGDSGGP
HVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKARVGPTSETPRLTHP
PY

BDBM50324743

n/a

Name

BDBM50324743

Synonyms:

(3R,4R)-1-(2,2-DIFLUORO-ETHYL)-PYRROLIDINE-3,4-DICARBOXYLIC ACID 3-[(5-CHLORO-PYRIDIN-2-YL)-AMIDE]-4-{[2-FLUORO-4-(2-OXO-2H-PYRIDIN-1-YL)-PHENYL]-AMIDE} | (3R,4R)-N3-(5-chloropyridin-2-yl)-1-(2,2-difluoroethyl)-N4-(2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)pyrrolidine-3,4-dicarboxamide | CHEMBL1221913

Type

Small organic molecule

Emp. Form.

C24H21ClF3N5O3

Mol. Mass.

519.903

SMILES

FC(F)CN1C[C@@H]([C@H](C1)C(=O)Nc1ccc(cc1F)-n1ccccc1=O)C(=O)Nc1ccc(Cl)cn1 |r|

Structure