Table 3.
Shc SH2 domain-binding affinities of bis N-olefin containing peptides.
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Peptide A Analogues | Peptide B Analogues | |||||||
No. | Positiona,b | n | IC50 ± s.d. (μM)c | No. | Positiona,b | n | IC50 ± s.d. (μM)c | |
31 | 0 | 1 | 189 ± 15 | 38 | 0 | 1 | 91 ± 12 | |
32 | 1 | 1 | 353 ± 34 | 39 | 1 | 1 | 81 ± 6 | |
33 | 2 | 1 | 48 ± 2 | 40 | 2 | 1 | 47 ± 2 | |
34 | 3 | 1 | 41 ± 7 | 41 | 3 | 1 | 450 ± 38 | |
35 | 0 | 2 | 165 ± 4 | 42 | 0 | 2 | 84 ± 4 | |
36 | 1 | 2 | 89 ± 5 | 43 | 1 | 2 | 84 ± 6 | |
37 | 2 | 2 | 8 ± 2 | 44 | 2 | 2 | 14 ± 3 |
Site of N-allyl substitution.
A designation of “0” indicates the lack of N-allyl substitution.
Determined by a fluorescence anisotropy based competition assay using peptide 8 as a reference as described in the experimental procedures.