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21844464831
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more..
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12
-
-
65149106189
-
-
note
-
2, 0.1 mg/ml BSA, at room temperature. Compounds, titrated in DMSO, were evaluated at eleven concentrations ranging from 50 μM to 0.2 nM. Reactions were incubated for 1 h at room temperature and were stopped by a 5-μl addition of EDTA (to 33 mM). A further addition of 5 μl detection reagents (for final 7 nM Streptavidin-APC (Perkin-Elmer #CR130-150), 1 nM Europium-labeled anti-phosphotyrosine monoclonal antibody (Perkin-Elmer #AD0067), added in reaction buffer (without DTT), was required for signal generation. After 30 minutes, signal was read on Perkin-Elmer Viewlux microplate imager or Wallac Victor fluorometer as subtracted from all samples for background).
-
-
-
-
13
-
-
65149086407
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-
US2007043068-A1, 2007
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Arnold, W. D.; Bounaud, P.; Gosberg, A.; Li, Z.; McDonald, I.; Steensma, R. W.; Wilson, M. E. US2007043068-A1, 2007.
-
-
-
Arnold, W.D.1
Bounaud, P.2
Gosberg, A.3
Li, Z.4
McDonald, I.5
Steensma, R.W.6
Wilson, M.E.7
-
14
-
-
65149083641
-
-
Arnold, W. D.; Bounaud, P.; Gosberg, A.; Li, Z.; McDonald, I.; Steensma, R. W.; Wilson, M. E. WO2006015123-A1, 2006.
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Arnold, W. D.; Bounaud, P.; Gosberg, A.; Li, Z.; McDonald, I.; Steensma, R. W.; Wilson, M. E. WO2006015123-A1, 2006.
-
-
-
-
15
-
-
65149098744
-
-
WO Patent 2004101565-A2, A3, 2004
-
Graczyk, P.; Palmer, V.; Khan, A. WO Patent 2004101565-A2, A3, 2004.
-
-
-
Graczyk, P.1
Palmer, V.2
Khan, A.3
-
16
-
-
42949149240
-
-
For a recent discussion of crystal structures of 1H-pyrrolo[2,3-b]pyridines bound to protein kinases, see:
-
For a recent discussion of crystal structures of 1H-pyrrolo[2,3-b]pyridines bound to protein kinases, see:. Tsai J., et al. Proc. Natl. Acad. Sci. U.S.A. 105 (2008) 3041
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(2008)
Proc. Natl. Acad. Sci. U.S.A.
, vol.105
, pp. 3041
-
-
Tsai, J.1
-
17
-
-
65149100255
-
-
note
-
50) was determined by 4 parameter fit of data using XLfit (value of no cell control was subtracted from all samples for background).
-
-
-
-
18
-
-
65149093269
-
-
note
-
The cellular potencies of 19 and 21, reported in Table 1, were not determined.
-
-
-
-
19
-
-
0028582185
-
-
note
-
factor of 20% at 2.6 Å using REFMAC. Crystallographic data for the structure in Figure 1 have been deposited at PDB:3ETA.
-
-
-
-
20
-
-
5044236233
-
-
For kinase ATP binding pocket nomenclature, see:
-
For kinase ATP binding pocket nomenclature, see:. Vulpetti A., and Bosotti R. Il Farmaco 59 (2004) 759
-
(2004)
Il Farmaco
, vol.59
, pp. 759
-
-
Vulpetti, A.1
Bosotti, R.2
-
21
-
-
65149106298
-
-
note
-
Compound 23 inhibited cellular proliferation in a COLO205 cell line with EC50 at 274 nM (average of 4 measurements).
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-
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