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PDBsum entry 4na7
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Hydrolase/hydrolase inhibitor
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PDB id
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4na7
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References listed in PDB file
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Key reference
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Title
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Tetrahydroquinoline derivatives as potent and selective factor xia inhibitors.
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Authors
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M.L.Quan,
P.C.Wong,
C.Wang,
F.Woerner,
J.M.Smallheer,
F.A.Barbera,
J.M.Bozarth,
R.L.Brown,
M.R.Harpel,
J.M.Luettgen,
P.E.Morin,
T.Peterson,
V.Ramamurthy,
A.R.Rendina,
K.A.Rossi,
C.A.Watson,
A.Wei,
G.Zhang,
D.Seiffert,
R.R.Wexler.
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Ref.
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J Med Chem, 2014,
57,
955-969.
[DOI no: ]
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PubMed id
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Abstract
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Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the
potential to demonstrate robust efficacy with a low bleeding risk profile.
Herein, we describe a series of tetrahydroquinoline (THQ) derivatives as FXIa
inhibitors. Compound 1 was identified as a potent and selective tool compound
for proof of concept studies. It exhibited excellent antithrombotic efficacy in
rabbit thrombosis models and did not prolong bleeding times. This demonstrates
proof of concept for the FXIa mechanism in animal models with a reversible,
small molecule inhibitor.
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