Table 5.
IC50 values of the non-proteogenic modifications of CSP2 analogs against the ComD1 and ComD2 receptorsa
| ComD1 | ComD2 | |||||
|---|---|---|---|---|---|---|
| Peptide Number | Peptide Name | Sequence | IC50 (nM)b | 95% CIc | IC50 (nM)b | 95% CIc |
| 33 | CSP2-E1AI4Nvad10 | AMRNvaSRIILdFLFLRKK | >1000 | -- | 42.2 | 34.1–52.0 |
| 34 | CSP2-E1AI4Nled10 | AMRNleSRIILdFLFLRKK | >1000 | -- | 79.1 | 74.7–84.0 |
| 35 | CSP2-E1AI4HLeud10 | AMRhLeuSRIILdFLFLRKK | >1000 | -- | 97.6 | 62.3–151 |
| 36 | CSP2-E1AI4NvaI8FL9RF13LL14Q | AMRNvaSRIFRDFLLQRKK | >1000 | -- | >1000 | — |
| 37 | CSP2-E1AI4NvaI8FL9Rd10F13LL14Q | AMRNvaSRIFRdFLLQRKK | --d | -- | 229 | 89.7–585 |
a
See experimental section for detail of reporter strains. See supporting information for methods and plots of antagonism dose response curves. All assays were performed in triplicates.
b
IC50 values were determined by testing peptides over a range of concentrations.
c
95% confidence interval.
d
IC50 not determined due to the analog’s low activity in primary antagonism screening assay.