Table 1. EC50/IC50 values of the alanine and D-amino acid scan analogs of CSP1 against ComD1 and ComD2 receptorsa.
| Name | EC50/IC50 (nM)b (95% CIc) | Name | EC50/IC50 (nM) (95% CI) | ||
|---|---|---|---|---|---|
|
|
|
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| ComD1 | ComD2 | ComD1 | ComD2 | ||
| CSP1 | 10.3 (6.27 - 16.8) | 526 (498 - 556) | CSP2 | 1650 (1190 - 2300) | 50.7 (40.6 - 63.2) |
|
| |||||
| CSP1-E1A | 85.7 (50.8 - 145)* | -- | CSP1-e1 | -- | -- |
| CSP1-M2A | 91.0 (75.4 - 110) | -- | CSP1-m2 | -- | -- |
| CSP1-R3A | --d | -- | CSP1-r3 | -- | -- |
| CSP1-L4A | 205 (179 - 235) | -- | CSP1-l4 | 628 (493 - 799) | -- |
| CSP1-S5A | -- | -- | CSP1-s5 | 10.0 (8.39 - 12.0) | -- |
| CSP1-K6A | 51.0 (37.9 - 68.6) | 24.0 (14.7 - 39.3) | CSP1-k6 | 147 (107 - 200) | 545 (482 - 616) |
| CSP1-F7A | -- | -- | CSP1-f7 | 506 (335 - 765) | 115 (96.2 - 137) |
| CSP1-F8A | >1,000 | -- | CSP1-f8 | 794 (610 - 1030) | >1000 |
| CSP1-R9A | 34.1 (29.9 - 38.7) | 646 (376 - 1110) | CSP1-r9 | -- | 304 (258 - 358) |
| CSP1-D10A | 54.3 (41.5 - 71.1) | 874 (560 - 1360) | CSP1-d10 | 107 (90.9 - 127) | 156 (134 - 181) |
| CSP1-F11A | -- | -- | CSP1-f11 | -- | -- |
| CSP1-I12A | 500 (199 - 1260) | -- | CSP1-i12 | 631 (547 - 728) | >1000 |
| CSP1-L13A | -- | -- | CSP1-l13 | 125 (99.1 - 158) | -- |
| CSP1-Q14A | -- | >1000 | CSP1-q14 | 12.2 (7.74 - 19.2) | -- |
| CSP1-R15A | 16.8 (12.8 - 22.1) | >1000 | CSP1-r15 | 8.37 (7.13 - 9.83) | -- |
| CSP1-K16A | 18.9 (10.0 - 35.6) | >1000 | CSP1-k16 | 8.10 (5.97 - 11.0) | -- |
| CSP1-K17A | 14.2 (6.23 - 32.5) | >1000 | CSP1-k17 | 5.88 (4.23 - 8.16) | >1000 |
a
See experimental section for detail of reporter strains and methods. See supporting information for plots of agonism or antagonism dose response curves. All assays performed in triplicate.
b
EC50 or IC50 values determined by testing peptides over a range of concentrations.
c
95% confidence interval.
d
EC50 not determined due to the analog's low induction in primary agonism screening assay. See supporting information for detail.
*
IC50 value.