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Lee, J.C.5
Young, P.R.6
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3
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84992535220
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Poconos, PA
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Lee, J. C.; Blumenthal, M. J.; Laydon, J. T.; Tan, K. B.; DeWitt, D. L. 7th International Conference of the Inflammatory Research Association; Poconos, PA, 1994. Lin, W. W.; Chen, B. C. Br. J. Pharmacol. 1999, 126, 1419.
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Lee, J.C.1
Blumenthal, M.J.2
Laydon, J.T.3
Tan, K.B.4
Dewitt, D.L.5
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4
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0033002192
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Lee, J. C.; Blumenthal, M. J.; Laydon, J. T.; Tan, K. B.; DeWitt, D. L. 7th International Conference of the Inflammatory Research Association; Poconos, PA, 1994. Lin, W. W.; Chen, B. C. Br. J. Pharmacol. 1999, 126, 1419.
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Lin, W.W.1
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5
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0030426902
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Badger, A. M.; Bradbeer, J. N.; Votta, B.; Lee, J. C.; Adams, J. L.; Griswold, D. E. J. Pharmacol. Exp. Ther. 1996, 279, 1453. Lee, J. C.; Kassis, S.; Kumar, S.; Badger, A.; Adams, Jerry L. Pharmacol. Ther. 1999, 82, 389.
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Adams, J.L.5
Griswold, D.E.6
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6
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0033030207
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Badger, A. M.; Bradbeer, J. N.; Votta, B.; Lee, J. C.; Adams, J. L.; Griswold, D. E. J. Pharmacol. Exp. Ther. 1996, 279, 1453. Lee, J. C.; Kassis, S.; Kumar, S.; Badger, A.; Adams, Jerry L. Pharmacol. Ther. 1999, 82, 389.
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Lee, J.C.1
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0343954188
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1: GP054086. Fitzi, K. DE 2221546, 1972
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1: GP054086. Fitzi, K. DE 2221546, 1972; Chem. Abstr. 1972, 78, 58428.
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9
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84992598006
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A phosphorylated form of His-p38α MAP kinase (10 ng/well) of murine origin was used and immobilised GST-ATF-2 as substrate in the presence of 120 μM cold ATP
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A phosphorylated form of His-p38α MAP kinase (10 ng/well) of murine origin was used and immobilised GST-ATF-2 as substrate in the presence of 120 μM cold ATP.
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-
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10
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84992606941
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COX-1 from ram seminal vesicles (Nr. 60100; Cayman Chemical Company) was used and PGE2 determined by RIA
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COX-1 from ram seminal vesicles (Nr. 60100; Cayman Chemical Company) was used and PGE2 determined by RIA.
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11
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0034642482
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Shewchuk, L.; Hassell, A.; Wisely, B.; Rocque, W.; Holmes, W.; Veal, J.; Kuyper, L. F. J. Med. Chem. 2000, 43, 133. Lisnock, J. M.; Tebben, A.; Frantz, B.; O'Neill, E. A.; Croft, G.; O'Keefe, S. J.; Li, B.; Hacker, C.; de Laszlo, S.; Smith, A.; Libby, B.; Liverton, N.; Hermes, J.; LoGrasso, P. Biochemistry 1998, 37, 16573.
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Shewchuk, L.1
Hassell, A.2
Wisely, B.3
Rocque, W.4
Holmes, W.5
Veal, J.6
Kuyper, L.F.7
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12
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0032564311
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Shewchuk, L.; Hassell, A.; Wisely, B.; Rocque, W.; Holmes, W.; Veal, J.; Kuyper, L. F. J. Med. Chem. 2000, 43, 133. Lisnock, J. M.; Tebben, A.; Frantz, B.; O'Neill, E. A.; Croft, G.; O'Keefe, S. J.; Li, B.; Hacker, C.; de Laszlo, S.; Smith, A.; Libby, B.; Liverton, N.; Hermes, J.; LoGrasso, P. Biochemistry 1998, 37, 16573.
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Lisnock, J.M.1
Tebben, A.2
Frantz, B.3
O'Neill, E.A.4
Croft, G.5
O'Keefe, S.J.6
Li, B.7
Hacker, C.8
De Laszlo, S.9
Smith, A.10
Libby, B.11
Liverton, N.12
Hermes, J.13
Lograsso, P.14
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13
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84992597993
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Human peripheral blood mononuclear cells from healthy volunteers were incubated with the inhibitor and stimulated with LPS/IFN-γ for 3 h. The supernatants were collected for TNF-α determination by ELISA
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Human peripheral blood mononuclear cells from healthy volunteers were incubated with the inhibitor and stimulated with LPS/IFN-γ for 3 h. The supernatants were collected for TNF-α determination by ELISA.
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14
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84992629622
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Eight-week old female OF1 mice were dosed perorally by gavage with solutions of the compounds in DMSO/cornoil. One hour after dosing, LPS (20 mg/kg) was injected iv for stimulation of TNF-α release into plasma. One h later blood was collected and TNF-α was determined using a mouse specific ELISA
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Eight-week old female OF1 mice were dosed perorally by gavage with solutions of the compounds in DMSO/cornoil. One hour after dosing, LPS (20 mg/kg) was injected iv for stimulation of TNF-α release into plasma. One h later blood was collected and TNF-α was determined using a mouse specific ELISA.
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15
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84992634900
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Compound 8 was dosed at 1 mg/kg iv and 20 mg/kg po. Compound 11 was dosed at 3 mg/kg iv and 10 mg/kg po
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Compound 8 was dosed at 1 mg/kg iv and 20 mg/kg po. Compound 11 was dosed at 3 mg/kg iv and 10 mg/kg po.
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16
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84992567135
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Cmax: maximal plasma concentration after oral dose (8: 20 mg/kg po. 11 mg/kg po)
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Cmax: maximal plasma concentration after oral dose (8: 20 mg/kg po. 11 mg/kg po).
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17
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84992634895
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AA: adjuvant induced arthritis. Female Wistar rats were immunized with Mycobacterium tuberculosis at day 0 and dosed with the compounds (2×25 mg/kg po per day) from day 14-20. Swelling of the joints was measured on day 20
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AA: adjuvant induced arthritis. Female Wistar rats were immunized with Mycobacterium tuberculosis at day 0 and dosed with the compounds (2×25 mg/kg po per day) from day 14-20. Swelling of the joints was measured on day 20.
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18
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84992594518
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CIA:collagen induced arthritis. Female (WAG×BUF/F1) rats were immunized intradermally with bovine nasal septum type II collagen emulsified in Freund's incomplete adjuvant. Compound 11 was dosed twice daily for 10 days after the onset of swelling
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CIA:collagen induced arthritis. Female (WAG×BUF/F1) rats were immunized intradermally with bovine nasal septum type II collagen emulsified in Freund's incomplete adjuvant. Compound 11 was dosed twice daily for 10 days after the onset of swelling.
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19
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84992598074
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Phosphorylated forms of His-p38β2, His-p38δ, His-JNK1 and His-JNK2 MAP kinases of human origin phosporylated the immobilised substrate GST-ATF-2 in the presence of cold ATP (120 μM). Antibody detected phosphorylated GST-ATF-2
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Phosphorylated forms of His-p38β2, His-p38δ, His-JNK1 and His-JNK2 MAP kinases of human origin phosporylated the immobilised substrate GST-ATF-2 in the presence of cold ATP (120 μM). Antibody detected phosphorylated GST-ATF-2.
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20
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84992613397
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32P)γ-ATP
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32P)γ-ATP.
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22
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0032541986
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Adams J.L., Boehm J.C., Kassis S., Gorycki P.D., Webb E.F., Hall R., Sorenson M., Lee J.C., Ayrton A., Griswold D.E., Gallagher T.F. Bioorg. Med. Chem. Lett. 8:1998;3111.
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Sorenson, M.7
Lee, J.C.8
Ayrton, A.9
Griswold, D.E.10
Gallagher, T.F.11
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23
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17644437502
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Gallagher T.F., Seibel G.L., Kassis S., Laydon J.T., Blumenthal M.J., Lee J.C., Lee D., Boehm J.C., Fier-Thompson S.M.et al. Bioorg. Med. Chem. 5:1997;49.
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Lee, J.C.6
Lee, D.7
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Fier-Thompson, S.M.9
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0005787022
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WO 9901449, 1999
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De Laszlo, S. E.; Chang, L. L.; Kim, D.; Mantlo, Nathan B. WO 9716442, 1997; Chem. Abstr. 1997, 127, 50543.
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