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References listed in PDB file
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Key reference
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Title
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Pyridazine and pyridazinone derivatives as potent and selective factor xia inhibitors.
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Authors
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Z.Hu,
C.Wang,
W.Han,
K.A.Rossi,
J.M.Bozarth,
Y.Wu,
S.Sheriff,
J.E.Myers,
J.M.Luettgen,
D.A.Seiffert,
R.R.Wexler,
M.L.Quan.
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Ref.
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Bioorg Med Chem Lett, 2018,
28,
987-992.
[DOI no: ]
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PubMed id
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Abstract
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Pyridazine and pyridazinone derivatives were designed and synthesized as
coagulation factor XIa inhibitors. Potent and selective inhibitors with single
digit nanomolar affinity for factor XIa were discovered. Selected inhibitors
demonstrated moderate oral bioavailability.
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Secondary reference #1
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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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Secondary reference #2
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Title
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Phenylimidazoles as potent and selective inhibitors of coagulation factor xia with in vivo antithrombotic activity.
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Authors
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J.J.Hangeland,
T.J.Friends,
K.A.Rossi,
J.M.Smallheer,
C.Wang,
Z.Sun,
J.R.Corte,
T.Fang,
P.C.Wong,
A.R.Rendina,
F.A.Barbera,
J.M.Bozarth,
J.M.Luettgen,
C.A.Watson,
G.Zhang,
A.Wei,
V.Ramamurthy,
P.E.Morin,
G.S.Bisacchi,
S.Subramaniam,
P.Arunachalam,
A.Mathur,
D.A.Seiffert,
R.R.Wexler,
M.L.Quan.
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Ref.
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J Med Chem, 2014,
57,
9915-9932.
[DOI no: ]
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PubMed id
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Secondary reference #3
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Title
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Pyridine and pyridinone-Based factor xia inhibitors.
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Authors
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J.R.Corte,
T.Fang,
J.J.Hangeland,
T.J.Friends,
A.R.Rendina,
J.M.Luettgen,
J.M.Bozarth,
F.A.Barbera,
K.A.Rossi,
A.Wei,
V.Ramamurthy,
P.E.Morin,
D.A.Seiffert,
R.R.Wexler,
M.L.Quan.
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Ref.
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Bioorg Med Chem Lett, 2015,
25,
925-930.
[DOI no: ]
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PubMed id
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Secondary reference #4
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Title
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Structure-Based design of inhibitors of coagulation factor xia with novel p1 moieties.
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Authors
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D.J.Pinto,
J.M.Smallheer,
J.R.Corte,
E.J.Austin,
C.Wang,
T.Fang,
L.M.Smith,
K.A.Rossi,
A.R.Rendina,
J.M.Bozarth,
G.Zhang,
A.Wei,
V.Ramamurthy,
S.Sheriff,
J.E.Myers,
P.E.Morin,
J.M.Luettgen,
D.A.Seiffert,
M.L.Quan,
R.R.Wexler.
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Ref.
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Bioorg Med Chem Lett, 2015,
25,
1635-1642.
[DOI no: ]
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PubMed id
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Secondary reference #5
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Title
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Discovery of a potent parenterally administered factor xia inhibitor with hydroxyquinolin-2(1h)-One as the p2' Moiety.
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Authors
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Z.Hu,
P.C.Wong,
P.J.Gilligan,
W.Han,
K.B.Pabbisetty,
J.M.Bozarth,
E.J.Crain,
T.Harper,
J.M.Luettgen,
J.E.Myers,
V.Ramamurthy,
K.A.Rossi,
S.Sheriff,
C.A.Watson,
A.Wei,
J.J.Zheng,
D.A.Seiffert,
R.R.Wexler,
M.L.Quan.
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Ref.
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Acs Med Chem Lett, 2015,
6,
590-595.
[DOI no: ]
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PubMed id
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Secondary reference #6
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Title
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Novel phenylalanine derived diamides as factor xia inhibitors.
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Authors
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L.M.Smith,
M.J.Orwat,
Z.Hu,
W.Han,
C.Wang,
K.A.Rossi,
P.J.Gilligan,
K.B.Pabbisetty,
H.Osuna,
J.R.Corte,
A.R.Rendina,
J.M.Luettgen,
P.C.Wong,
R.Narayanan,
T.W.Harper,
J.M.Bozarth,
E.J.Crain,
A.Wei,
V.Ramamurthy,
P.E.Morin,
B.Xin,
J.Zheng,
D.A.Seiffert,
M.L.Quan,
P.Y.Lam,
R.R.Wexler,
D.J.Pinto.
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Ref.
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Bioorg Med Chem Lett, 2016,
26,
472-478.
[DOI no: ]
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PubMed id
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Secondary reference #7
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Title
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Orally bioavailable pyridine and pyrimidine-Based factor xia inhibitors: discovery of the methyl n-Phenyl carbamate p2 prime group.
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Authors
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J.R.Corte,
T.Fang,
D.J.Pinto,
M.J.Orwat,
A.R.Rendina,
J.M.Luettgen,
K.A.Rossi,
A.Wei,
V.Ramamurthy,
J.E.Myers,
S.Sheriff,
R.Narayanan,
T.W.Harper,
J.J.Zheng,
Y.X.Li,
D.A.Seiffert,
R.R.Wexler,
M.L.Quan.
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Ref.
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Bioorg Med Chem Lett, 2016,
24,
2257-2272.
[DOI no: ]
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PubMed id
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Secondary reference #8
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Title
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Structure-Based design of macrocyclic factor xia inhibitors: discovery of the macrocyclic amide linker.
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Authors
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J.R.Corte,
T.Fang,
H.Osuna,
D.J.Pinto,
K.A.Rossi,
J.E.Myers,
S.Sheriff,
Z.Lou,
J.J.Zheng,
T.W.Harper,
J.M.Bozarth,
Y.Wu,
J.M.Luettgen,
D.A.Seiffert,
C.P.Decicco,
R.R.Wexler,
M.L.Quan.
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Ref.
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J Med Chem, 2017,
60,
1060-1075.
[DOI no: ]
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PubMed id
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Secondary reference #9
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Title
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Macrocyclic inhibitors of factor xia: discovery of alkyl-Substituted macrocyclic amide linkers with improved potency.
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Authors
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J.R.Corte,
W.Yang,
T.Fang,
Y.Wang,
H.Osuna,
A.Lai,
W.R.Ewing,
K.A.Rossi,
J.E.Myers,
S.Sheriff,
Z.Lou,
J.J.Zheng,
T.W.Harper,
J.M.Bozarth,
Y.Wu,
J.M.Luettgen,
D.A.Seiffert,
M.L.Quan,
R.R.Wexler,
P.Y.S.Lam.
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Ref.
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Bioorg Med Chem Lett, 2017,
27,
3833-3839.
[DOI no: ]
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PubMed id
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Secondary reference #10
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Title
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Macrocyclic factor xia inhibitors.
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Authors
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C.Wang,
J.R.Corte,
K.A.Rossi,
J.M.Bozarth,
Y.Wu,
S.Sheriff,
J.E.Myers,
J.M.Luettgen,
D.A.Seiffert,
R.R.Wexler,
M.L.Quan.
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Ref.
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Bioorg Med Chem Lett, 2017,
27,
4056-4060.
[DOI no: ]
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PubMed id
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Secondary reference #11
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Title
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Discovery of a parenteral small molecule coagulation factor xia inhibitor clinical candidate (bms-962212).
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Authors
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D.J.P.Pinto,
M.J.Orwat,
L.M.Smith,
M.L.Quan,
P.Y.S.Lam,
K.A.Rossi,
A.Apedo,
J.M.Bozarth,
Y.Wu,
J.J.Zheng,
B.Xin,
N.Toussaint,
P.Stetsko,
O.Gudmundsson,
B.Maxwell,
E.J.Crain,
P.C.Wong,
Z.Lou,
T.W.Harper,
S.A.Chacko,
J.E.Myers,
S.Sheriff,
H.Zhang,
X.Hou,
A.Mathur,
D.A.Seiffert,
R.R.Wexler,
J.M.Luettgen,
W.R.Ewing.
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Ref.
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J Med Chem, 2017,
60,
9703-9723.
[DOI no: ]
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PubMed id
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