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. Author manuscript; available in PMC: 2018 Jun 16.
Published in final edited form as: Org Lett. 2017 Jun 7;19(12):3295–3298. doi: 10.1021/acs.orglett.7b01444

Table 1.

EC50 values for the alanine scan, D-amino acid scan, and tail modification analogues of GBAP against the FsrC receptora

peptide name EC50b [95% CI]c (nM)
GBAP 1.15 [0.825–1.59]
GBAP-Q1A 0.549 [0.299–1.01]
GBAP-N2A 0.704 [0.522–0.898]
GBAP-P4A 0.270 [0.202–0.360]
GBAP-N5A 341 [200–581]
GBAP-I6Af > 1,000
GBAP-F7Af > 1,000
GBAP-G8A > 10,000
GBAP-Q9A 312 [222–437]
GBAP-W10A 246 [117–520]
GBAP-M11A 164 [93.8–288]
GBAP-q1d 0.211 [0.0798–0.599]
GBAP-n2 0.304 [0.168–0.552]
GBAP-s3 45.1 [17.0–120]
GBAP-p4 > 1,000
GBAP-n5 > 1,000
GBAP-i6 > 1,000
GBAP-f7 4.97 [3.12–7.77]
GBAP-q9 > 1,000
GBAP-w10 > 10,000
GBAP-m11 231 [129–414]
Ac-GBAP 1.50 [1.31–1.73]
GBAP-DesQ1 1.26 [1.15–1.39]
Ac-GBAP-DesQ1 1.44 [0.855–2.44]
GBAP-DesQ1N2 lactame,f > 10,000
Ac-GBAP-DesQ1N2 1.01 [0.496–2.06]
a

See Supporting Information for details of reporter strain and methods. See Supporting Information for plots of agonism dose response curves. All assays performed in triplicate. The full sequences for the peptides can be found in Table S-5.

b

EC50 values determined by testing peptides over a range of concentrations.

c

95% confidence interval.

d

lower case letters indicate residues replaced with the D-enantiomer.

e

Lactam (head-to-tail) cyclization.

f

Weak inhibitor.