-
1
-
-
33644671816
-
-
Spooren, W.; Riemer, C.; Meltzer, H. Nat. Rev. Drug Disc. 2005, 4, 967.
-
(2005)
Nat. Rev. Drug Disc.
, vol.4
, pp. 967
-
-
Spooren, W.1
Riemer, C.2
Meltzer, H.3
-
4
-
-
58549115885
-
-
See for example: (a)
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See for example: (a) Smith, P. W.; Wyman, P. A.; Lovell, P.; Goodacre, C.; Serafinokwska, H. T.; Vong, A.; Harrington, F.; Flynn, S.; Bradley, D. M.; Porter, R.; Coggon, S.; Murkitt, G.; Searle, K.; Thomas, D. R.; Watson, J. M.; Martin, W.; Wu, Z.; Dawson, L. Bioorg. Med. Chem. Lett. 2009, 19, 837;
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 837
-
-
Smith, P.W.1
Wyman, P.A.2
Lovell, P.3
Goodacre, C.4
Serafinokwska, H.T.5
Vong, A.6
Harrington, F.7
Flynn, S.8
Bradley, D.M.9
Porter, R.10
Coggon, S.11
Murkitt, G.12
Searle, K.13
Thomas, D.R.14
Watson, J.M.15
Martin, W.16
Wu, Z.17
Dawson, L.18
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5
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33749441299
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(b) Elliott, J. M.; Carling, R. W.; Chambers, M.; Chicchi, G. G.; Hutson, P. H.; Jones, A. B.; MacLeod, A.; Marwood, R.; Mensese-Lorente, G.; Mezzogori, E.; Murray, F.; Rigby, M.; Royo, I.; Russell, M. G. N.; Sohal, B.; Tsao, K. L.; Williams, B. Bioorg. Med. Chem. Lett. 2006, 16, 5748;
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 5748
-
-
Elliott, J.M.1
Carling, R.W.2
Chambers, M.3
Chicchi, G.G.4
Hutson, P.H.5
Jones, A.B.6
MacLeod, A.7
Marwood, R.8
Mensese-Lorente, G.9
Mezzogori, E.10
Murray, F.11
Rigby, M.12
Royo, I.13
Russell, M.G.N.14
Sohal, B.15
Tsao, K.L.16
Williams, B.17
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6
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79960959242
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doi:10.1016/j.bmcl.2010.11.003
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(c) Xiong, H.; Kang, J.; Woods, J. M.; McCauley, J. P., Jr.; Koether, G. M.; Albert, J. S.; Hinkley, L.; Gadient, R. A.; Simpson, T. R. Bioorg. Med. Chem. Lett. 2010. doi:10.1016/j.bmcl.2010.11.003.
-
(2010)
Bioorg. Med. Chem. Lett.
-
-
Xiong, H.1
Kang, J.2
Woods, J.M.3
McCauley Jr., J.P.4
Koether, G.M.5
Albert, J.S.6
Hinkley, L.7
Gadient, R.A.8
Simpson, T.R.9
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7
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0036194079
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2+] causes a conformational change in the aequorin protein thereby eliciting a quantifiable luminescent signal. This method is adapted to detect agonist, antagonist or allosteric modulators of receptor activity
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2+] causes a conformational change in the aequorin protein thereby eliciting a quantifiable luminescent signal. This method is adapted to detect agonist, antagonist or allosteric modulators of receptor activity.
-
(2002)
J. Biomol. Screen.
, vol.7
, pp. 57
-
-
Le Poul, E.1
Hisada, S.2
Mizuguchi, Y.3
Dupriez, V.J.4
Burgeon, E.5
Detheux, M.6
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8
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0010505654
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-
Petruso, S.; Caronna, S.; Sferlazzo, M.; Sprio, V. J. Heterocycl. Chem. 1990, 27, 1277.
-
(1990)
J. Heterocycl. Chem.
, vol.27
, pp. 1277
-
-
Petruso, S.1
Caronna, S.2
Sferlazzo, M.3
Sprio, V.4
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10
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79952490349
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note
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Given the good agreement between the radioligand binding and aequorin functional assays, the latter set of results will be principally used in foregoing SAR discussions.
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11
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0037030653
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Veber, D. F.; Johnson, S. R.; Cheng, H. Y.; Smith, B. R.; Ward, K. W.; Kopple, K. D. J. Med. Chem. 2002, 45, 2615.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2615
-
-
Veber, D.F.1
Johnson, S.R.2
Cheng, H.Y.3
Smith, B.R.4
Ward, K.W.5
Kopple, K.D.6
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12
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79952487514
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No appreciable solubility difference between 4 and 5 was detectable at pH 7, although at pH 5 benzylpiperazine analog 5 was decidedly more soluble
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No appreciable solubility difference between 4 and 5 was detectable at pH 7, although at pH 5 benzylpiperazine analog 5 was decidedly more soluble.
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13
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79952487806
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C log P values cited herein are calculated using ChemBioDraw (CambridgeSoft, v.12)
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C log P values cited herein are calculated using ChemBioDraw (CambridgeSoft, v.12).
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14
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84882088781
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Academic Press: Burlington, Massachusetts, Chapter 12
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Kerns, E. H.; Di, L. Drug-like Properties: Concepts, Structure Design and Methods: From ADME to Toxicity Optimization; Academic Press: Burlington, Massachusetts, 2008. Chapter 12.
-
(2008)
Drug-like Properties: Concepts, Structure Design and Methods: From ADME to Toxicity Optimization
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Kerns, E.H.1
Di, L.2
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15
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5244332801
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Talnetant was made and characterized as per: (a) Osanetant was purchased from Charnwood Molecular, UK. It was made and characterized as per
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Talnetant was made and characterized as per: (a) Giardina, G. A. M.; Sarau, H. M.; Farina, C.; Medhurst, A. D.; Grugni, M.; Foley, J. J.; Raveglia, L. F.; Schmidt, D. B.; Rigolio, R.; Vassallo, M.; Vecchietti, V.; Hay, D. W. P. J. Med. Chem. 1996, 39, 2281; Osanetant was purchased from Charnwood Molecular, UK. It was made and characterized as per:
-
(1996)
J. Med. Chem.
, vol.39
, pp. 2281
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Giardina, G.A.M.1
Sarau, H.M.2
Farina, C.3
Medhurst, A.D.4
Grugni, M.5
Foley, J.J.6
Raveglia, L.F.7
Schmidt, D.B.8
Rigolio, R.9
Vassallo, M.10
Vecchietti, V.11
Hay, D.W.P.12
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16
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0030575607
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(b) Giardina, G. A. M.; Grugni, M.; Rigolio, R.; Vassllo, M.; Erhard, K.; Farina, C. Bioorg. Med. Chem. Lett. 1996, 6, 2307;
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 2307
-
-
Giardina, G.A.M.1
Grugni, M.2
Rigolio, R.3
Vassllo, M.4
Erhard, K.5
Farina, C.6
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17
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0031552139
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(c) Chen, H. G.; Chung, F.-Z.; Goel, O. P.; Kesten, J. S.; Knobelsdorf, J.; Lee, H. T.; Rubin, J. R. Bioorg. Med. Chem. Lett. 1997, 7, 555.
-
(1997)
Bioorg. Med. Chem. Lett.
, vol.7
, pp. 555
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Chen, H.G.1
Chung, F.-Z.2
Goel, O.P.3
Kesten, J.S.4
Knobelsdorf, J.5
Lee, H.T.6
Rubin, J.R.7
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18
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15144349599
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For a report on the pharmacokinetic profile of talnetant, see Tables 2 and 3 The reported values in Table 5 herein are in agreement with those in the cited reference
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For a report on the pharmacokinetic profile of talnetant, see Tables 2 and 3 in: Sarau, H. M.; Griswold, D. E.; Potts, W.; Foley, J. J.; Schmidt, D. B.; Webb, E. F.; Martin, L. D.; Brawner, M. E.; Elshourbagy, N. A.; Medhurst, A. M.; Giardina, G. A. M.; Hay, D. W. P. J. Pharmacol. Exp. Ther. 1997, 281, 1303. The reported values in Table 5 herein are in agreement with those in the cited reference.
-
(1997)
J. Pharmacol. Exp. Ther.
, vol.281
, pp. 1303
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Sarau, H.M.1
Griswold, D.E.2
Potts, W.3
Foley, J.J.4
Schmidt, D.B.5
Webb, E.F.6
Martin, L.D.7
Brawner, M.E.8
Elshourbagy, N.A.9
Medhurst, A.M.10
Giardina, G.A.M.11
Hay, D.W.P.12
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19
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55549146766
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For example: Compound 7 (GSK183390A) in the cited reference is depicted below and has been reported to have a clean 7-day toxicology profile in rats with no safety issues. (Chemical Equation Presented)
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For example: Martres, P.; Faucher, N.; Laroze, A.; Pineau, O.; Fouchet, M.-H.; Potvain, F.; Grillot, D.; Beneton, V. Bioorg. Med. Chem. Lett. 2008, 18, 6251. Compound 7 (GSK183390A) in the cited reference is depicted below and has been reported to have a clean 7-day toxicology profile in rats with no safety issues. (Chemical Equation Presented)
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 6251
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Martres, P.1
Faucher, N.2
Laroze, A.3
Pineau, O.4
Fouchet, M.-H.5
Potvain, F.6
Grillot, D.7
Beneton, V.8
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