. Author manuscript; available in PMC: 2015 Jan 11.

Published in final edited form as: J Med Chem. 2010 Jul 22;53(14):5179–5185. doi: 10.1021/jm100139b

Table 3.

Binding Affinities of Peptide Analogues of Ac-ARA-NH₂ Designed to Investigate the Role of Intramolecular Hydrogen Bonds

peptide	formula	IC₅₀ ± SD (µM)	K_i ± SD (µM)
Ac-10mer	Ac-ARAEVHLRKS-NH₂	0.02 ± 0.004	0.003 ± 0.001
H₂N-10mer	H₂N-ARAEVHLRKS-NH₂	34 ± 3	7.30 ± 0.70
Ac-3mer	Ac-ARA-NH₂	0.54 ± 0.03	0.12 ± 0.01
H₂N-3mer	H₂N-ARA-NH₂	> 300	> 50
CHO-3mer	CHO-ARA-NH₂	14.9 ± 1.4	3.20 ± 0.3
Δ1	Ac-AR-(N-Me)A-NH₂	> 300	> 50
Δ2a	Ac-ARA-CONHMe	0.70 ± 0.14	0.15 ± 0.03
Δ2b	Ac-ARA-CONMe₂	30 ± 5	6.50 ± 1.20
Δ2c	Ac-ARA-COOCH₃	7.30 ± 0.80	1.60 ± 0.20