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. Author manuscript; available in PMC: 2022 Sep 9.
Published in final edited form as: J Med Chem. 2021 Aug 20;64(17):13038–13053. doi: 10.1021/acs.jmedchem.1c01130

Table 1.

Sequences of Hits Derived from the 2ND Generation Library

graphic file with name nihms-1735248-t0002.jpg
Peptide Hit Sequence HTRF IC50 (μM)a MTT EC50 (μM)a
X4 X3 X2 X1
B3-4 β-Ala β-Ala Lys none 4.4 ± 1.3 29 ± 6
B3-4-1 D-Tyr Asp Ser D-Val NA NT
B3-4-2 D-Glu His D-Pro D-Tyr 5.8 ± 1.1 NA
B3-4-3 D-Thr Ser D-Pro Pip 8.0 ± 1.0 NT
B3-4-4 (B4) Orn D-Arg Fpa D-Ala 1.7 ± 0.2 17 ± 4
B3-4-5 D-Thr His D-Glu D-Arg 6.9 ± 2.1 NT
B3-4-6 Ser Gln Ile D-Arg 9.7 ± 0.8 NT
B3-4-7 Gly Gln D-Leu D-Arg 1.7 ± 0.6 NA
B3-4-8 D-Leu Ser D-Nal D-Arg 18 ± 4 NT
B3-4-9 D-Asn D-Val D-Thr D-Trp NA NT
B3-4-10 D-Pro D-Arg D-Phe D-Tyr NA NT
B3-4-11 Nle Gly Nle D-Arg 7.2 ± 2.0 24 ± 7
B3-4-12 Ala D-Arg D-Phe Fpa 3.1 ± 0.6 19 ± 6
B3-4-13 Orn D-Arg D-β-homoAla Fpa 1.7 ± 0.1 30 ± 11
B3-4-14 D-Lys His D-Tyr D-Glu NA NT
B3-4-15 Orn D-Val D-β-homoAla D-Trp 2.9 ± 0.8 NA
B3-4-16 D-Pro D-Arg D-Nal D-Glu NA NT
B3-4-17 Orn D-Asn D-Tyr D-Thr 5.7 ± 0.1 NA
a

Values reported represent the mean ± SD of 3 or more independent experiments. NA, no significant activity; NT, not tested.