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. Author manuscript; available in PMC: 2010 Nov 1.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Sep 9;19(21):6122–6126. doi: 10.1016/j.bmcl.2009.09.010

Table 1.

IC50 determinations for inhibiting EphB3 phosphorylation of BTK-peptide

graphic file with name nihms153223t1.jpg
Cmpd X Y R1 R2 Method IC50
(µM)
1 C=O NH 2-Cl-Ph H --- 1.0
34 C=O NH Ph H A NA
35 C=O NH 2-F-Ph H A ~ 20
36 C=O NH 3-Cl-Ph H A NA
37 C=O NH 4-Cl-Ph H A NA
38 C=O NH 2,3-Cl2-Ph H A ~20
39 C=O NH 2-OMe-Ph H A NA
40 C=O NH 2-CF3-Ph H A > 20
41 C=O NH 2-CN-Ph H A > 20
42 C=O NH 2-MeSO2Ph H A NA
43 C=O NMe 2-Cl-Ph H A NA
44 C=O NH CH2-2-Cl-Ph H A NA
7 NH C=O 2-Cl-Ph H B > 20
45 CH2 NH 2-Cl-Ph H A > 20
46 C=O NH 2-Cl-Ph 4-Me C ~ 15
47 C=O NH 2-Cl-Ph 5-Me C 0.26
48 C=O NH 2-Cl-Ph 6-Me C ~ 15
49 C=O NH 2-Cl-Ph 7-Me C NA
50 C=O NH 2-Cl-Ph 4-Cl C ~ 20
51 C=O NH 2-Cl-Ph 5-Cl C 2.0
52 C=O NH 2-Cl-Ph 6-Cl C > 20
53 C=O NH 2-Cl-Ph 5-OMe C 0.19
54 C=O NH 2-Cl-Ph 5-Ph C 0.066
55 C=O NH 2-Cl-Ph 5-NMe2 C 0.077
56 C=O NH 2-Cl-Ph 5-Pyrr D 0.20
57 C=O NH 2-Cl-Ph 5-Morph D 0.24
58 C=O NH 2-Cl-Ph 5-Pip D 0.063
59 C=O NH 2-Cl-Ph 5-OBn C ~ 20

NA: Not active at 20 µM; Pyrr = N-pyrrolidinyl; Morph = N-morpholinyl; Pip = N-piperidinyl