Table 3.
Name | EC50 (nM)b | 95% CIc | Fold changed | Name | EC50 (nM)b | 95% CIc | Fold changed |
---|---|---|---|---|---|---|---|
21-CSP | 240 | 200 – 290 | 18-CSP | 6.2 | 3.7 – 10.0 | ||
21-CSP-des-S1 | 23 | 19 – 28 | 0.10 | 18-CSP-des-S1 | 4.8 | 2.3 – 10.0 | 0.77 |
21-CSP-des-S1G2 | 120 | 49 – 310 | 0.50 | 18-CSP-des-S1G2 | 7.9 | 4.1 – 15 | 1.3 |
21-CSP-des-S1G2S3 | 530 | 340 – 810 | 2.2 | 18-CSP-des-S1G2S3 | 85 | 46 – 160 | 14 |
21-CSP-des-S1G2S3L4 | 3600 | 1500 – 8900 | 15 | 18-CSP-des-S1G2S3L4 | 570 | 270 – 1200 | 92 |
21-CSP-des-S1G2S3L4S5 | 3300 | 1600 – 6900 | 14 | 18-CSP-des-S1G2S3L4S5 | 950 | 460 – 2000 | 150 |
21-CSP-des-K21 | 98 | 52 – 180 | 0.41 | 18-CSP-des-A18 | --e | -- | -- |
21-CSP-des-G20K21 | 3600 | 2100 – 6100 | 15 | 18-CSP-des-Q17A18 | --e | -- | -- |
21-CSP-S3T | 94 | 76 – 120 | 0.39 | 18-CSP-S3T | 2.1 | 1.0 – 4.2 | 0.34 |
18-CSP-s1s3l4 | 17 | 11 – 26 | 2.7 | ||||
18-CSP-s1s3l4L10AR13AS14A | 3.4 | 2.9 – 4.00 | 0.55 | ||||
18-CSP-S1AL10AR13AS14A | 1.7 | 0.90 – 3.3 | 0.27 |
See experimental section for details on the reporter strain and methods. See supporting information for primary screening assay results and plots of agonism dose response curves. All assays performed in triplicate.
EC50 values determined by testing peptides over a range of concentrations.
95% confidence interval.
Ratio where each analog’s EC50 is divided by native CSP EC50; a value <1 indicates a better activator than the parent CSP.
EC50 not determined due to the analog’s low induction in primary agonism screening assay.