-
4
-
-
79952717349
-
-
G. Raghu, H.R. Collard, J.J. Egan, F.J. Martinez, J. Behr, K.K. Brown, T.V. Colby, J.-F. Cordier, K.R. Flaherty, J.A. Lasky, D.A. Lynch, J.H. Ryu, J.J. Swigris, A.U. Wells, J. Ancochea, D. Bouros, C. Carvalho, U. Costabel, M. Ebina, D.M. Hansell, T. Johkoh, D.S. Kim, T.E. King Jr., Y. Kondoh, F. Myers, N.L. Müller, A.G. Nicholson, L. Richeldi, M. Selman, R.F. Dudden, B.S. Griss, S.L. Protzko, and H.L. Schünemann Am. J. Respir. Crit. Care Med. 183 2011 788
-
(2011)
Am. J. Respir. Crit. Care Med.
, vol.183
, pp. 788
-
-
Raghu, G.1
Collard, H.R.2
Egan, J.J.3
Martinez, F.J.4
Behr, J.5
Brown, K.K.6
Colby, T.V.7
Cordier, J.-F.8
Flaherty, K.R.9
Lasky, J.A.10
Lynch, D.A.11
Ryu, J.H.12
Swigris, J.J.13
Wells, A.U.14
Ancochea, J.15
Bouros, D.16
Carvalho, C.17
Costabel, U.18
Ebina, M.19
Hansell, D.M.20
Johkoh, T.21
Kim, D.S.22
King, Jr.T.E.23
Kondoh, Y.24
Myers, F.25
Müller, N.L.26
Nicholson, A.G.27
Richeldi, L.28
Selman, M.29
Dudden, R.F.30
Griss, B.S.31
Protzko, S.L.32
Schünemann, H.L.33
more..
-
5
-
-
84862790560
-
-
Plantevin Krenitsky, V., Nadolny, L., Sahasrabudhe, K., Ayala, L., Delgado, M., Clareen, S., Hilgraf, R., Albers, R., Kois, A., Hughes, K., Wright, J., Sudbeck, E., Ghosh, S., Nowakowski, J., Muir, J., Cathers, B., Giegel, D., Xu, L., Celeridad, M., Moghaddam, M., Khatsenko, O., Omholt, P., Pai, S., Fan, R., Tang, Y., Shirley, M. A., Benis, B., Blease, K., Raymon, H., Bhagwat, S., Henderson, I., Cole, A. G., Bennett, B., Satoh, Y. Preceding article
-
Plantevin Krenitsky, V., Nadolny, L., Sahasrabudhe, K., Ayala, L., Delgado, M., Clareen, S., Hilgraf, R., Albers, R., Kois, A., Hughes, K., Wright, J., Sudbeck, E., Ghosh, S., Nowakowski, J., Muir, J., Cathers, B., Giegel, D., Xu, L., Celeridad, M., Moghaddam, M., Khatsenko, O., Omholt, P., Pai, S., Fan, R., Tang, Y., Shirley, M. A., Benis, B., Blease, K., Raymon, H., Bhagwat, S., Henderson, I., Cole, A. G., Bennett, B., Satoh, Y. Preceding article.
-
-
-
-
7
-
-
0347949530
-
-
P.R. Eynott, P. Nath, S.-Y. Leung, I.M. Adcock, B.L. Bennett, and K.F. Chung Br. J. Pharmacol. 140 2003 1373
-
(2003)
Br. J. Pharmacol.
, vol.140
, pp. 1373
-
-
Eynott, P.R.1
Nath, P.2
Leung, S.-Y.3
Adcock, I.M.4
Bennett, B.L.5
Chung, K.F.6
-
8
-
-
73349139523
-
-
M.H. de Borst, J. Prakash, M. Sandovici, P.A. Klok, I. Hamming, R.J. Kok, G. Navis, and H. van Goor J. Pharmacol. Exp. Ther. 331 2009 896
-
(2009)
J. Pharmacol. Exp. Ther.
, vol.331
, pp. 896
-
-
De Borst, M.H.1
Prakash, J.2
Sandovici, M.3
Klok, P.A.4
Hamming, I.5
Kok, R.J.6
Navis, G.7
Van Goor, H.8
-
9
-
-
72249114470
-
-
J. Kluwe, J.-P. Pradere, G.-Y. Gwak, A. Mencin, S. De Minicis, C.H. Osterreicher, J. Colmenero, R. Bataller, and R.F. Schwabe Gastroenterology 138 2010 347
-
(2010)
Gastroenterology
, vol.138
, pp. 347
-
-
Kluwe, J.1
Pradere, J.-P.2
Gwak, G.-Y.3
Mencin, A.4
De Minicis, S.5
Osterreicher, C.H.6
Colmenero, J.7
Bataller, R.8
Schwabe, R.F.9
-
10
-
-
78751632066
-
-
W. Wu, A. Muchir, J. Shan, G. Bonne, and Howard J. Worman Circulation 123 2011 53
-
(2011)
Circulation
, vol.123
, pp. 53
-
-
Wu, W.1
Muchir, A.2
Shan, J.3
Bonne, G.4
Worman, H.J.5
-
11
-
-
35349026241
-
-
M.H. De Borst, J. Prakash, W.B.W.H. Melenhorst, M.C. van den Heuvel, R.J. Kok, G. Navis, and H. van Goor J. Pathol. 213 2007 219
-
(2007)
J. Pathol.
, vol.213
, pp. 219
-
-
De Borst, M.H.1
Prakash, J.2
Melenhorst, W.B.W.H.3
Van Den Heuvel, M.C.4
Kok, R.J.5
Navis, G.6
Van Goor, H.7
-
15
-
-
34848921683
-
-
M. Morgenthaler, E. Schweizer, A. Hoffmann-Röder, F. Benini, R.E. Martin, G. Jaeschke, B. Wagner, H. Fischer, S. Bendels, D. Zimmerli, J. Schneider, F. Diederich, M. Kansy, and K. Müller ChemMedChem 2 2007 1100
-
(2007)
ChemMedChem
, vol.2
, pp. 1100
-
-
Morgenthaler, M.1
Schweizer, E.2
Hoffmann-Röder, A.3
Benini, F.4
Martin, R.E.5
Jaeschke, G.6
Wagner, B.7
Fischer, H.8
Bendels, S.9
Zimmerli, D.10
Schneider, J.11
Diederich, F.12
Kansy, M.13
Müller, K.14
-
16
-
-
84862780110
-
-
Experimental details on biochemical and cellular assays can be found in the Supplementary data section
-
Experimental details on biochemical and cellular assays can be found in the Supplementary data section.
-
-
-
-
19
-
-
19944399431
-
-
A.S. Kalgutkar, I. Gardner, R.S. Obach, C.L. Shaffer, E. Callegari, K.R. Henne, A.E. Mutlib, D.K. Dalvie, J.S. Lee, Y. Nakai, J.P. O'Donnell, J. Boer, and S.P. Harriman Curr. Drug Met. 6 2005 161
-
(2005)
Curr. Drug Met.
, vol.6
, pp. 161
-
-
Kalgutkar, A.S.1
Gardner, I.2
Obach, R.S.3
Shaffer, C.L.4
Callegari, E.5
Henne, K.R.6
Mutlib, A.E.7
Dalvie, D.K.8
Lee, J.S.9
Nakai, Y.10
O'Donnell, J.P.11
Boer, J.12
Harriman, S.P.13
-
20
-
-
84862780109
-
-
This class of compounds is 8-10 times more potent in JNK2 and JNK3 than JNK1
-
This class of compounds is 8-10 times more potent in JNK2 and JNK3 than JNK1.
-
-
-
-
21
-
-
84862790559
-
-
Model for the assessment of the potential anti-inflammatory effects of therapeutic agents on acute cytokine production by measuring the effect of a compound administered by oral gavage, on the release of plasma tumor necrosis factor (TNF)-α following lipopolysaccharide (LPS) injection. See Supplementary data for details
-
Model for the assessment of the potential anti-inflammatory effects of therapeutic agents on acute cytokine production by measuring the effect of a compound administered by oral gavage, on the release of plasma tumor necrosis factor (TNF)-α following lipopolysaccharide (LPS) injection. See Supplementary data for details.
-
-
-
-
22
-
-
84862795036
-
-
The JNK3 isoform was the only one available to us for crystallography during this drug discovery program
-
The JNK3 isoform was the only one available to us for crystallography during this drug discovery program.
-
-
-
-
23
-
-
84862780112
-
-
All images were generated using using The PyMOL Molecular Graphics System, Version 1.3, Schrödinger, LLC
-
All images were generated using using The PyMOL Molecular Graphics System, Version 1.3, Schrödinger, LLC.
-
-
-
-
24
-
-
84862785114
-
-
The PDB deposition code for 1 JNK3 complex crystal structure is 3TTI
-
The PDB deposition code for 1 JNK3 complex crystal structure is 3TTI.
-
-
-
-
25
-
-
84862780111
-
-
See Supplementary data for details
-
See Supplementary data for details.
-
-
-
-
26
-
-
84862827128
-
-
Reddy Mehvar Chirality and Drug Design and Development Marcel Dekker Inc. New York Chapter 8
-
N.M. Davies Reddy Mehvar Chiral Inversion Chirality and Drug Design and Development 2004 Marcel Dekker Inc. New York 351 392 Chapter 8
-
(2004)
Chiral Inversion
, pp. 351-392
-
-
Davies, N.M.1
-
27
-
-
0037013428
-
-
A similar trend was observed prior to the profiling of 1 with compounds containing cis-hydroxy cyclohexyl amine at the C2 position. See also
-
A similar trend was observed prior to the profiling of 1 with compounds containing cis-hydroxy cyclohexyl amine at the C2 position. See also: M.Y. Chu-Moyer, W.E. Ballinger, D.A. Beebe, J.B. Coutcher, W.W. Day, J. Li, P.J. Oates, and R.M. Weekly Bioorg. Med. Chem. Lett. 12 2002 1477
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 1477
-
-
Chu-Moyer, M.Y.1
Ballinger, W.E.2
Beebe, D.A.3
Coutcher, J.B.4
Day, W.W.5
Li, J.6
Oates, P.J.7
Weekly, R.M.8
-
28
-
-
84862785112
-
-
Note
-
The percentage of the cis isomer was calculated in vivo based on the po AUC. The major isomerization in mouse and rat hepatocytes translated in the in vivo formation of 20% and 200%, respectively of the cis isomer. On the other hand, the isomerization in dog was below limit of detection in vitro and tracked with a 1.5% formation in vivo. Trace isomerization in monkey resulted in trace formation in vivo as well. A similar profile was observed with analogs containing a trans-hydroxy cyclohexyl amine at C2.
-
-
-
-
29
-
-
84856225788
-
-
Y. Ye, L. Kong, M. Assaf, L. Liu, A. Wu, H. Lau, S. Choudhury, and O. Laskin Clin. Pharmacol. Ther. 89 2011 31
-
(2011)
Clin. Pharmacol. Ther.
, vol.89
, pp. 31
-
-
Ye, Y.1
Kong, L.2
Assaf, M.3
Liu, L.4
Wu, A.5
Lau, H.6
Choudhury, S.7
Laskin, O.8
-
30
-
-
84862785113
-
-
Trial Identifier NCT01203943
-
www.clinicaltrials.gov; Trial Identifier NCT01203943.
-
-
-
|