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7
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55749114279
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note
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d is the dissociation constant for pGA = 240 nM.
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8
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0037131187
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9
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55749112366
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Akt lum assay: non-small cell lung carcinoma cell line H1299 was cultured in DMEM + 10%FBS, 10,000 cells/well were cultured in 96-well plate. Compounds were added to each well starting at 10 μM with threefold serial dilution of 11 points of various concentration. Twenty-four hours post adding compounds, cell lysates were prepared and subjected to Luminex 100 system using the Beadlyte Akt/PKB kit-Upstate #46-605.
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Akt lum assay: non-small cell lung carcinoma cell line H1299 was cultured in DMEM + 10%FBS, 10,000 cells/well were cultured in 96-well plate. Compounds were added to each well starting at 10 μM with threefold serial dilution of 11 points of various concentration. Twenty-four hours post adding compounds, cell lysates were prepared and subjected to Luminex 100 system using the Beadlyte Akt/PKB kit-Upstate #46-605.
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10
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0030863995
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Grenert J.P., Sullivan W.P., Fadden P., Haysead T.A., Clark J., Mimnaugh E., Krutzsch H., Ochel H.-J., Schulte T.W., Sausville E., Neckers L.M., and Toft D.O. J. Biol. Chem. 272 (1997) 23843
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Krutzsch, H.7
Ochel, H.-J.8
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Sausville, E.10
Neckers, L.M.11
Toft, D.O.12
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11
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0035071607
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13
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21244505104
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Drysdale, M.J.13
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15
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38349157746
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Brough P.A., Aherne W., Barril X., Borgognoni J., Boxall K., Cansfield K.-M., Cheung J., Collins I., Davies N.G.M., Drysdale M.J., Dymock B., Eccles S.A., Finch H., Fink A., Hayes A., Howes R., Hubbard R.E., James K., Jordan A.M., Lockie A., Martins V., Massey A., Mattews T.P., McDonald E., Northfield C.J., Pearl L.H., Prodromou C., Ray S., Raynaud F.I., Roughley S.D., Sharp S.Y., Surgenor A., Walmsley D.L., Webb P., Wood M., Workman P., and Wright L. J. Med. Chem. 51 (2008) 196
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Eccles, S.A.12
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Fink, A.14
Hayes, A.15
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Hubbard, R.E.17
James, K.18
Jordan, A.M.19
Lockie, A.20
Martins, V.21
Massey, A.22
Mattews, T.P.23
McDonald, E.24
Northfield, C.J.25
Pearl, L.H.26
Prodromou, C.27
Ray, S.28
Raynaud, F.I.29
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Walmsley, D.L.33
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more..
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16
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39149136212
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Gopalsamy A., Shi M., Goals J., Vogan E., Jacob J., Johnson M., Lee F., Nilakantan R., Petersen R., Svenson K., Chopra R., Tam M.S., Wen Y., Ellingboe J., Arndt K., and Boschelli F. J. Med. Chem. 51 (2008) 373
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18
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55749103111
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The work on optimization of compound 7 will be described in a latter manuscript.
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The work on optimization of compound 7 will be described in a latter manuscript.
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19
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55749093456
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The SAR was done with racemic compounds due to difficulty making chiral pure compounds.
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The SAR was done with racemic compounds due to difficulty making chiral pure compounds.
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21
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0034710542
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Clarke P.A., Hostein I., Banerji U., Stefano F.D., Maloney A., Walton M., Judson I., and Workman P. Oncogene 19 (2000) 4125
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Walton, M.6
Judson, I.7
Workman, P.8
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