-
3
-
-
33644783643
-
-
N. Kertesz, V. Krasnoperov, R. Reddy, L. Leshanski, S.R. Kumar, S. Zozulya, and P.S. Gill Blood 107 2006 2330
-
(2006)
Blood
, vol.107
, pp. 2330
-
-
Kertesz, N.1
Krasnoperov, V.2
Reddy, R.3
Leshanski, L.4
Kumar, S.R.5
Zozulya, S.6
Gill, P.S.7
-
4
-
-
77950577414
-
-
V. Krasnoperov, S.R. Kumar, E. Ley, X. Li, J. Scehnet, R. Liu, S. Zozulya, and P.S. Gill Am. J. Pathol. 176 2010 2029
-
(2010)
Am. J. Pathol.
, vol.176
, pp. 2029
-
-
Krasnoperov, V.1
Kumar, S.R.2
Ley, E.3
Li, X.4
Scehnet, J.5
Liu, R.6
Zozulya, S.7
Gill, P.S.8
-
5
-
-
77953029002
-
-
Y. Wang, M. Nakayama, M.E. Pitulescu, T.S. Schmidt, M.L. Bochenek, A. Sakakibara, S. Adams, A. Davy, U. Deutsch, U. Luethi, A. Barberis, L.E. Benjamin, T. Maekinen, C.D. Nobes, and R.H. Adams Nature 465 2010 483
-
(2010)
Nature
, vol.465
, pp. 483
-
-
Wang, Y.1
Nakayama, M.2
Pitulescu, M.E.3
Schmidt, T.S.4
Bochenek, M.L.5
Sakakibara, A.6
Adams, S.7
Davy, A.8
Deutsch, U.9
Luethi, U.10
Barberis, A.11
Benjamin, L.E.12
Maekinen, T.13
Nobes, C.D.14
Adams, R.H.15
-
6
-
-
78149412006
-
-
G. Martiny-Baron, P. Holzer, E. Billy, C. Schnell, J. Brueggen, M. Ferretti, N. Schmiedeberg, J.M. Wood, P. Furet, and P. Imbach Angiogenesis 13 2010 259
-
(2010)
Angiogenesis
, vol.13
, pp. 259
-
-
Martiny-Baron, G.1
Holzer, P.2
Billy, E.3
Schnell, C.4
Brueggen, J.5
Ferretti, M.6
Schmiedeberg, N.7
Wood, J.M.8
Furet, P.9
Imbach, P.10
-
7
-
-
43049114977
-
-
C. Bardelle, D. Cross, S. Davenport, J.G. Kettle, E.J. Ko, A.G. Leach, A. Mortlock, J. Read, N.J. Roberts, P. Robins, and E.J. Williams Bioorg. Med. Chem. Lett. 18 2008 2776
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 2776
-
-
Bardelle, C.1
Cross, D.2
Davenport, S.3
Kettle, J.G.4
Ko, E.J.5
Leach, A.G.6
Mortlock, A.7
Read, J.8
Roberts, N.J.9
Robins, P.10
Williams, E.J.11
-
8
-
-
54049137918
-
-
C. Bardelle, T. Coleman, D. Cross, S. Davenport, J.G. Kettle, E.J. Ko, A.G. Leach, A. Mortlock, J. Read, N.J. Roberts, P. Robins, and E.J. Williams Bioorg. Med. Chem. Lett. 18 2008 5717
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 5717
-
-
Bardelle, C.1
Coleman, T.2
Cross, D.3
Davenport, S.4
Kettle, J.G.5
Ko, E.J.6
Leach, A.G.7
Mortlock, A.8
Read, J.9
Roberts, N.J.10
Robins, P.11
Williams, E.J.12
-
9
-
-
77957857898
-
-
C. Bardelle, B. Barlaam, N. Brooks, T. Coleman, D. Cross, R. Ducray, I. Green, C. Lambert-van der Brempt, A. Olivier, and J. Read Bioorg. Med. Chem. Lett. 20 2010 6242
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 6242
-
-
Bardelle, C.1
Barlaam, B.2
Brooks, N.3
Coleman, T.4
Cross, D.5
Ducray, R.6
Green, I.7
Lambert-Van Der Brempt, C.8
Olivier, A.9
Read, J.10
-
10
-
-
71849113647
-
-
S.A. Mitchell, M.D. Danca, P.A. Blomgren, J.W. Darrow, K.S. Currie, J.E. Kropf, S.H. Lee, S.L. Gallion, J.-M. Xiong, D.A. Pippin, R.W. DeSimone, D.R. Brittelli, D.C. Eustice, A. Bourret, M. Hill-Drzewi, P.M. Maciejewski, and L.L. Elkin Bioorg. Med. Chem. Lett. 19 2009 6991
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6991
-
-
Mitchell, S.A.1
Danca, M.D.2
Blomgren, P.A.3
Darrow, J.W.4
Currie, K.S.5
Kropf, J.E.6
Lee, S.H.7
Gallion, S.L.8
Xiong, J.-M.9
Pippin, D.A.10
Desimone, R.W.11
Brittelli, D.R.12
Eustice, D.C.13
Bourret, A.14
Hill-Drzewi, M.15
MacIejewski, P.M.16
Elkin, L.L.17
-
11
-
-
70350072332
-
-
K. Lafleur, D. Huang, T. Zhou, A. Caflisch, and C. Nevado J. Med. Chem. 52 2009 6433
-
(2009)
J. Med. Chem.
, vol.52
, pp. 6433
-
-
Lafleur, K.1
Huang, D.2
Zhou, T.3
Caflisch, A.4
Nevado, C.5
-
12
-
-
67649996707
-
-
Y. Choi, F. Syeda, J.R. Walker, P.J. Finerty, D. Cuerrier, A. Wojciechowski, Q. Liu, S. Dhe-Paganon, and N.S. Gray Bioorg. Med. Chem. Lett. 19 2009 4467
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4467
-
-
Choi, Y.1
Syeda, F.2
Walker, J.R.3
Finerty, P.J.4
Cuerrier, D.5
Wojciechowski, A.6
Liu, Q.7
Dhe-Paganon, S.8
Gray, N.S.9
-
13
-
-
38049018155
-
-
See Supplementary data in: M.W. Karaman, S. Herrgard, D.K. Treiber, P. Gallant, C.E. Atteridge, B.T. Campbell, K.W. Chan, P. Ciceri, M.I. Davis, P.T. Edeen, R. Faraoni, M. Floyd, J.P. Hunt, D.J. Lockhart, Z.V. Milanov, M.J. Morrison, G. Pallares, H.K. Patel, S. Pritchard, L.M. Wodicka, and P.P. Zarrinkar Nat. Biotechnol. 26 2008 127
-
(2008)
Nat. Biotechnol.
, vol.26
, pp. 127
-
-
Karaman, M.W.1
Herrgard, S.2
Treiber, D.K.3
Gallant, P.4
Atteridge, C.E.5
Campbell, B.T.6
Chan, K.W.7
Ciceri, P.8
Davis, M.I.9
Edeen, P.T.10
Faraoni, R.11
Floyd, M.12
Hunt, J.P.13
Lockhart, D.J.14
Milanov, Z.V.15
Morrison, M.J.16
Pallares, G.17
Patel, H.K.18
Pritchard, S.19
Wodicka, L.M.20
Zarrinkar, P.P.21
more..
-
14
-
-
79953288497
-
-
note
-
The compounds described in reference 8 are also inhibitors of the VEGFR2 and Tie2 receptor tyrosine kinases, both of which are linked to angiogenic mechanisms.
-
-
-
-
16
-
-
79953268571
-
-
note
-
PCT international applications WO/2008-104754 (for compd 3-14, 18-32), WO/2008-132505 (for compd 33-34), and WO/2009-010794 (for compd 15-17).
-
-
-
-
18
-
-
0842304432
-
-
For a description of this assay see: P.A. Ple, T.P. Green, L.F. Hennequin, J. Curwen, M. Fennell, J. Allen, C. Lambert-van der Brempt, and G. Costello J. Med. Chem. 47 2004 871
-
(2004)
J. Med. Chem.
, vol.47
, pp. 871
-
-
Ple, P.A.1
Green, T.P.2
Hennequin, L.F.3
Curwen, J.4
Fennell, M.5
Allen, J.6
Lambert-Van Der Brempt, C.7
Costello, G.8
-
19
-
-
79953288759
-
-
note
-
In addition to ephB4, compound 12 is likely to inhibit other members of the Eph receptors family, given the high structural homology of their kinase domains.
-
-
-
-
20
-
-
79953280224
-
-
note
-
Time dependant inhibition (TDI) of CYP450 (isoforms 1A2, 2C9, 2C19, 2D6 and 3A4) was evaluated by pre-incubating the compound (10 μM) with human liver microsomes for 30 min in the presence vs. absence of NADPH, followed by incubation with a specific CYP substrate with NADPH. Compound 12 gave 50% TDI on CYP3A4 with no significant effect on the 4 other isoforms. In the same assay, 1 gave, respectively, 40% and 42% TDI against CYP2C9 and 3A4 and 2 gave 62% TDI against CYP3A4 (see Ref. 7).
-
-
-
-
23
-
-
79953270259
-
-
note
-
2, respectively.
-
-
-
|