Table 3.
Compound | Name | % inhibition at 320 μM | IC50 (μM)a |
---|---|---|---|
1 | p53 (17–26) b | 98 ± 2 | 8 ± 1 |
4a | Boc–WF–NH2 | No Inhibition | ND c |
4b | Boc–WF–N(CH2)5 | 13 ± 1 | ND c |
5a | Boc–RWF–NH2 | No Inhibition | ND c |
5b | Boc–RWF–N(CH2)5 | 42 ± 3 | 463 ± 45 |
6a | Boc–LRWF–NH2 | 14 ± 2 | ND c |
6b | Boc–LRWF–N(CH2)5 | 82 ± 4 | 192 ± 27 |
7a | Boc–DLRWF–NH2 | No Inhibition | ND c |
7b | Boc–DLRWF–N(CH2)5 | 13 ± 1 | ND c |
8 | c-(ADLRWF) | 12 ± 1 | ND c |
Calculated from weighted non-linear fits of dose-dependent responses (see Supporting Information for details).
KD of 1 has been reported to be 390 ± 20 nM (ref. 34).
Not determined due to low activity and poor solubility at high concentrations.