-
1
-
-
0030609068
-
-
G. Collo, S. Neidhart, E. Kawashima, M. Kosco-Vibois, R.A. North, and G. Buell Neuropharmacology 36 1997 1277
-
(1997)
Neuropharmacology
, vol.36
, pp. 1277
-
-
Collo, G.1
Neidhart, S.2
Kawashima, E.3
Kosco-Vibois, M.4
North, R.A.5
Buell, G.6
-
3
-
-
0023796357
-
-
H.P. Buisman, T.H. Steinberg, J. Fischbarg, S.C. Silverstein, S.A. Vogelzang, C. Ince, D.L. Ypey, and P.C. Leijh Proc. Natl. Acad. Sci. U.S.A. 85 1988 7988
-
(1988)
Proc. Natl. Acad. Sci. U.S.A.
, vol.85
, pp. 7988
-
-
Buisman, H.P.1
Steinberg, T.H.2
Fischbarg, J.3
Silverstein, S.C.4
Vogelzang, S.A.5
Ince, C.6
Ypey, D.L.7
Leijh, P.C.8
-
4
-
-
33646072818
-
-
D. Ferrari, C. Pizzirani, E. Adinolfi, R.M. Lemoli, A. Curti, M. Idzko, E. Panther, and F. Di Virgilio J. Immunol. 176 2006 3877
-
(2006)
J. Immunol.
, vol.176
, pp. 3877
-
-
Ferrari, D.1
Pizzirani, C.2
Adinolfi, E.3
Lemoli, R.M.4
Curti, A.5
Idzko, M.6
Panther, E.7
Di Virgilio, F.8
-
6
-
-
20144375454
-
-
I.P. Chessel, J.P. Hatcher, C. Bountra, A.D. Michel, J.P. Hughes, P. Green, J. Egerton, M. Murfin, J. Richardson, W.L. Peck, C.B.A. Grahames, M.A. Casula, Y. Yiangou, R. Birch, P. Anand, and G.N. Buell Pain 114 2005 386
-
(2005)
Pain
, vol.114
, pp. 386
-
-
Chessel, I.P.1
Hatcher, J.P.2
Bountra, C.3
Michel, A.D.4
Hughes, J.P.5
Green, P.6
Egerton, J.7
Murfin, M.8
Richardson, J.9
Peck, W.L.10
Grahames, C.B.A.11
Casula, M.A.12
Yiangou, Y.13
Birch, R.14
Anand, P.15
Buell, G.N.16
-
7
-
-
33751165071
-
-
P.M. Honore, D. Donnelly-Roberts, M. Namovic, G. Hsieh, C. Zhu, J. Mikusa, G. Hernandez, C. Zhong, D.M. Gauvin, P. Chandran, R. Harris, A.P. Medrano, W. Carroll, K. Marsh, J.P. Sullivan, C.R. Faltynek, and M.F. Jarvis J. Pharmacol. Exp. Ther. 319 2006 1376
-
(2006)
J. Pharmacol. Exp. Ther.
, vol.319
, pp. 1376
-
-
Honore, P.M.1
Donnelly-Roberts, D.2
Namovic, M.3
Hsieh, G.4
Zhu, C.5
Mikusa, J.6
Hernandez, G.7
Zhong, C.8
Gauvin, D.M.9
Chandran, P.10
Harris, R.11
Medrano, A.P.12
Carroll, W.13
Marsh, K.14
Sullivan, J.P.15
Faltynek, C.R.16
Jarvis, M.F.17
-
8
-
-
57349085122
-
-
D.C. Broom, D.J. Matson, E. Bradshaw, M.E. Buck, R. Meade, S. Coombs, M. Matchett, K.K. Ford, W. Yu, J. Yuan, S.H. Sun, R. Ochoa, J.E. Krause, D.J. Wustrow, and D.N. Cortright J. Pharmacol. Exp. Ther. 327 2008 620
-
(2008)
J. Pharmacol. Exp. Ther.
, vol.327
, pp. 620
-
-
Broom, D.C.1
Matson, D.J.2
Bradshaw, E.3
Buck, M.E.4
Meade, R.5
Coombs, S.6
Matchett, M.7
Ford, K.K.8
Yu, W.9
Yuan, J.10
Sun, S.H.11
Ochoa, R.12
Krause, J.E.13
Wustrow, D.J.14
Cortright, D.N.15
-
9
-
-
66249113481
-
-
A. Perez-Medrano, D.L. Donnelly-Roberts, P. Honore, G.C. Hsieh, M.T. Namovic, S. Peddi, Q. Shuai, Y. Wang, C.R. Faltynek, M.F. Jarvis, and W.A. Carroll J. Med. Chem. 52 2009 3366
-
(2009)
J. Med. Chem.
, vol.52
, pp. 3366
-
-
Perez-Medrano, A.1
Donnelly-Roberts, D.L.2
Honore, P.3
Hsieh, G.C.4
Namovic, M.T.5
Peddi, S.6
Shuai, Q.7
Wang, Y.8
Faltynek, C.R.9
Jarvis, M.F.10
Carroll, W.A.11
-
10
-
-
33745142545
-
-
D.W. Nelson, R.J. Gregg, M.E. Kort, A. Perez-Medrano, E.A. Voight, Y. Wang, G. Grayson, M.T. Namovic, D.L. Donnelly-Roberts, W. Niforatos, P. Honore, M.F. Jarvis, C.R. Faltynek, and W.A. Carroll J. Med. Chem. 49 2006 3659
-
(2006)
J. Med. Chem.
, vol.49
, pp. 3659
-
-
Nelson, D.W.1
Gregg, R.J.2
Kort, M.E.3
Perez-Medrano, A.4
Voight, E.A.5
Wang, Y.6
Grayson, G.7
Namovic, M.T.8
Donnelly-Roberts, D.L.9
Niforatos, W.10
Honore, P.11
Jarvis, M.F.12
Faltynek, C.R.13
Carroll, W.A.14
-
11
-
-
77955664743
-
-
I.B. McInnes, N.J. Snell, J.H. Perrett, H. Parmar, M.M. Wang, and C. Astbury Arthritis Rheum. [71st Annu Sci Meet Am Coll Rheumatol (Nov 6-11, Boston) 2007] 56 2007 Abst 2085
-
(2007)
Arthritis Rheum. [71st Annu Sci Meet Am Coll Rheumatol (Nov 6-11, Boston) 2007]
, vol.56
-
-
McInnes, I.B.1
Snell, N.J.2
Perrett, J.H.3
Parmar, H.4
Wang, M.M.5
Astbury, C.6
-
12
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77955658669
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ClinicalTrial.gov Identifier: NCT00628095
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ClinicalTrial.gov Identifier: NCT00628095.
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13
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77952105608
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L.J. Chambers, A.J. Stevens, A.P. Moses, A.D. Michel, B. Slingsby, D.S. Walter, D.J. Davies, D.J. Livermore, E. Fonfria, E.H. Demont, M. Vimal, P.J. Theobald, P.J. Beswick, R.J. Gleave, S.A. Roman, S. Senger, and S. Roomans Bioorg. Med. Chem. Lett. 20 2010 3161
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 3161
-
-
Chambers, L.J.1
Stevens, A.J.2
Moses, A.P.3
Michel, A.D.4
Slingsby, B.5
Walter, D.S.6
Davies, D.J.7
Livermore, D.J.8
Fonfria, E.9
Demont, E.H.10
Vimal, M.11
Theobald, P.J.12
Beswick, P.J.13
Gleave, R.J.14
Roman, S.A.15
Senger, S.16
Roomans, S.17
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14
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77955414233
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P.J. Beswick, A. Billinton, L.J. Chambers, D.K. Dean, E. Fonfria, R.J. Gleave, S.J. Medhurst, A.D. Michel, A.P. Moses, S. Patel, S.A. Roman, S. Roomans, S. Senger, A.J. Stevens, and D.S. Walter Bioorg. Med. Chem. Lett. 20 2010 4653
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 4653
-
-
Beswick, P.J.1
Billinton, A.2
Chambers, L.J.3
Dean, D.K.4
Fonfria, E.5
Gleave, R.J.6
Medhurst, S.J.7
Michel, A.D.8
Moses, A.P.9
Patel, S.10
Roman, S.A.11
Roomans, S.12
Senger, S.13
Stevens, A.J.14
Walter, D.S.15
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15
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77955654780
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max values of 100%. Full details of the assay protocol can be found in patent application WO 2007 141267 A1
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max values of 100%. Full details of the assay protocol can be found in patent application WO 2007 141267 A1.
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17
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77955660511
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Calculated log D values were obtained using ACD Labs software v8.0
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Calculated log D values were obtained using ACD Labs software v8.0.
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20
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67649962669
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The same concept was independently proposed by researchers at Pfizer and termed lipE. T. Ryckmans, M.P. Edwards, V.A. Horne, A. Monica Correia, D.R. Owen, L.R. Thompson, I. Tran, M.F. Tutt, and T. Young Bioorg. Med. Chem. Lett. 15 2009 4406
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 4406
-
-
Ryckmans, T.1
Edwards, M.P.2
Horne, V.A.3
Monica Correia, A.4
Owen, D.R.5
Thompson, L.R.6
Tran, I.7
Tutt, M.F.8
Young, T.9
-
22
-
-
0030938416
-
-
C.H. Hay, M.A. Trevethick, A. Wheeldon, J.S. Browers, and J.S. De Belleroche Neuroscience 78 1997 843
-
(1997)
Neuroscience
, vol.78
, pp. 843
-
-
Hay, C.H.1
Trevethick, M.A.2
Wheeldon, A.3
Browers, J.S.4
De Belleroche, J.S.5
-
23
-
-
33745346911
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-
A.W. Wilson, S.J. Medhurst, C.I. Dixon, N.C. Bontoft, L.A. Winyard, K.T. Brackenborough, J. De Alba, C.J. Clarke, M.J. Gunthorpe, G.A. Hicks, C. Bountra, D.S. McQueen, and I.P. Chessell Eur. J. Pain 10 2006 537
-
(2006)
Eur. J. Pain
, vol.10
, pp. 537
-
-
Wilson, A.W.1
Medhurst, S.J.2
Dixon, C.I.3
Bontoft, N.C.4
Winyard, L.A.5
Brackenborough, K.T.6
De Alba, J.7
Clarke, C.J.8
Gunthorpe, M.J.9
Hicks, G.A.10
Bountra, C.11
McQueen, D.S.12
Chessell, I.P.13
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24
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77955657829
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50 of greater than two- to threefold was considered to be significant and, depending on the baseline degree of inhibition, to potentially represent a developability risk
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50 of greater than two- to threefold was considered to be significant and, depending on the baseline degree of inhibition, to potentially represent a developability risk.
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25
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77955662349
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The overlay was generated using the software FLO (Thistlesoft, Colebrook, CT06021, USA)
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The overlay was generated using the software FLO (Thistlesoft, Colebrook, CT06021, USA).
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26
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77955653985
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24 and annotated with simple calculated properties (e.g., molecular weight, hydrogen-bond donor and acceptor counts)
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24 and annotated with simple calculated properties (e.g., molecular weight, hydrogen-bond donor and acceptor counts).
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27
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10044265608
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-
G. Harper, G.S. Bravi, S.D. Pickett, J. Hussain, and D.V.S. Green J. Chem. Inf. Comput. Sci. 446 2004 2145
-
(2004)
J. Chem. Inf. Comput. Sci.
, vol.446
, pp. 2145
-
-
Harper, G.1
Bravi, G.S.2
Pickett, S.D.3
Hussain, J.4
Green, D.V.S.5
-
28
-
-
0033523672
-
-
G. Schneider, W. Neidhart, T. Giller, and G. Schmid Angew. Chem., Int. Ed. 38 1999 2894
-
(1999)
Angew. Chem., Int. Ed.
, vol.38
, pp. 2894
-
-
Schneider, G.1
Neidhart, W.2
Giller, T.3
Schmid, G.4
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30
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77955658734
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Also see WO 2008/003697A1 for additional synthetic details
-
Also see WO 2008/003697A1 for additional synthetic details.
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31
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77955657047
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http://www.cerep.fr.
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32
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0031750861
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FeSSIF: Fed-state-simulated intestinal fluid. E. Galia, E. Nicolaides, D. Horter, R. Lobenberg, C. Reppas, and J.B. Dressman Pharm. Res. 15 1998 698
-
(1998)
Pharm. Res.
, vol.15
, pp. 698
-
-
Galia, E.1
Nicolaides, E.2
Horter, D.3
Lobenberg, R.4
Reppas, C.5
Dressman, J.B.6
-
33
-
-
77955659941
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All experiments were performed in accordance with the United Kingdom Animals (Scientific Procedures) Act, 1986 under Project Licence as well as under the review and approval of the GlaxoSmithKline Procedures Review Panel. GlaxoSmithKline safety regulations were adhered to at all times
-
All experiments were performed in accordance with the United Kingdom Animals (Scientific Procedures) Act, 1986 under Project Licence as well as under the review and approval of the GlaxoSmithKline Procedures Review Panel. GlaxoSmithKline safety regulations were adhered to at all times.
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