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77955656737
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Two isoforms of Rho-kinase (ROCK1 and ROCK2) are known and share >90% homology in the kinase domain. No significant differences in the SAR of the isoquinolone series between the two isoforms observed
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Two isoforms of Rho-kinase (ROCK1 and ROCK2) are known and share >90% homology in the kinase domain. No significant differences in the SAR of the isoquinolone series between the two isoforms observed.
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33845888587
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0037030653
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D. Veber, S. Johnson, H. Cheng, B. Smith, K. Ward, and K. Kopple J. Med. Chem. 45 2002 2615
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77955658338
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50 were determined for PRKG1 (230 nM), PRKCL2 (500 nM), p70S6 K (180 nM), and MSK2 (480 nM)
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50 were determined for PRKG1 (230 nM), PRKCL2 (500 nM), p70S6 K (180 nM), and MSK2 (480 nM).
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28
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77955661789
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PDB ID: 3NCZ
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PDB ID: 3NCZ.
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29
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77955662210
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Rat PK data was obtained from an IV cassette study (n = 3, 0.2 mg/kg) followed by an oral leg (n = 1, 10 mg/kg) in male Sprague-Dawley rats
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Rat PK data was obtained from an IV cassette study (n = 3, 0.2 mg/kg) followed by an oral leg (n = 1, 10 mg/kg) in male Sprague-Dawley rats.
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77955664911
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A recent report from researchers at GSK demonstrated that upon chronic dosing of a Rho-kinase inhibitor the bp lowering effects diminished over time. The efficacy of compound 20 has not been examined in similar multi-dose studies Washington, DC, Aug 16 paper MEDI 252
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A recent report from researchers at GSK demonstrated that upon chronic dosing of a Rho-kinase inhibitor the bp lowering effects diminished over time. The efficacy of compound 20 has not been examined in similar multi-dose studies. Goodman, K.; Dowdell, S.; Gaitanopoulos, D.; Ivy, R.; Sehon, C.; Stavenger, R.; Wang, G.; Viet, A.; Xu, W.; Ye, G.; Semus, S.; Evans, C.; Fries, H.; Jolivette, L.; Jung, D.; Wright, L.; Smith, G.; Behm, D.; Bentley, R.; Doe, C.; Hu, E.; Lee, D. 238th ACS National Meeting, Washington, DC, Aug 16, 2009; paper MEDI 252.
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238th ACS National Meeting
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Goodman, K.1
Dowdell, S.2
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Ivy, R.4
Sehon, C.5
Stavenger, R.6
Wang, G.7
Viet, A.8
Xu, W.9
Ye, G.10
Semus, S.11
Evans, C.12
Fries, H.13
Jolivette, L.14
Jung, D.15
Wright, L.16
Smith, G.17
Behm, D.18
Bentley, R.19
Doe, C.20
Hu, E.21
Lee, D.22
more..
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