Table 4.
IC50 values of the E1A & 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 |
| CSP2-E1Ad10e | AMRISRIILdFLFLRKK | >1000 | -- | 56.5 | 53.5–59.6 | |
| 25 | CSP2-E1AL9RL14Q | AMRISRIIRDFLFQRKK | >1000 | -- | --d | -- |
| 26 | CSP2-E1AL9Rd10L14Q | AMRISRIIRdFLFQRKK | --d | -- | --d | -- |
| 27 | CSP2-E1AI4LL9RL14Q | AMRLSRIIRDFLFQRKK | >1000 | -- | >1000 | -- |
| 28 | CSP2-E1AI4LL9Rd10L14Q | AMRLSRIIRdFLFQRKK | >1000 | -- | --d | -- |
| 29 | CSP2-E1AI4LL9RF13LL14Q | AMRLSRIIRDFLLQRKK | >1000 | -- | --d | -- |
| 30 | CSP2-E1AI4LL9Rd10F13LL14Q | AMRLSRIIRdFLLQRKK | >1000 | -- | 168 | 119–238 |
| 31 | CSP2-E1AI4LI8FL9RF13LL14Q | AMRLSRIFRDFLLQRKK | 455 | 270–767 | --d | -- |
| 32 | CSP2-E1AI4LI8FL9Rd10F13LL14Q | AMRLSRIFRdFLLQRKK | >1000 | -- | 161 | 135–193 |
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.
e
Data from ref. 28.