Table 6.
IC50 values of the E1A, I4Nva & d10 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 |
| 38 | CSP2-E1AI4NvaI8Fd10 | AMRNvaSRIFLdFLFLRKK | >1000 | -- | 42.9 | 16.7–110 |
| 39 | CSP2-E1AI4NvaL9Rd10 | AMRNvaSRIIRdFLFLRKK | >1000 | -- | 225 | 115–439 |
| 40 | CSP2-E1AI4Nvad10F13L | AMRNvaSRIILdFLLLRKK | >1000 | -- | 43.9 | 34.0–57.5 |
| 41 | CSP2-E1AI4Nvad10L14Q | AMRNvaSRIILdFLFQRKK | 510 | 416–625 | 18.2 | 10.8–30.5 |
| 42 | CSP2-E1AI4NvaI8FL9Rd10 | AMRNvaSRIFRdFLFLRKK | >1000 | -- | 41.6 | 22.4–77.0 |
| 43 | CSP2-E1AI4NvaI8Fd10F13L | AMRNvaSRIFLdFLLLRKK | >1000 | -- | 32.1 | 19.6–52.3 |
| 44 | CSP2-E1AI4NvaI8Fd10L14Q | AMRNvaSRIFLdFLFQRKK | >1000 | -- | 33.1 | 15.8–69.0 |
| 45 | CSP2-E1AI4NvaL9Rd10F13 | AMRNvaSRIIRdFLLLRKK | >1000 | -- | 407 | 176–940 |
| 46 | CSP2-E1AI4NvaL9Rd10L14Q | AMRNvaSRIIRdFLFQRKK | >1000 | -- | --d | -- |
| 47 | CSP2-E1AI4Nvad10F13LL14Q | AMRNvaSRIILdFLLQRKK | >1000 | -- | 53.5 | 39.4–73.0 |
| 48 | CSP2-E1AI4NvaI8FL9Rd10F13L | AMRNvaSRIFRdFLLLRKK | >1000 | -- | 183 | 77.2–436 |
| 49 | CSP2-E1AI4NvaI8FL9Rd10L14Q | AMRNvaSRIFRdFLFQRKK | >1000 | -- | 51.6 | 40.5–65.5 |
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. dIC50 not determined due to the analog’s low activity in primary antagonism screening assay.