Synthesis and Biological Evaluation of New CRH Analogues

Table 3

Binding affinities of h/r-CRH analogues.

	Analogues	Binding affinity^aIC50 (nM)
	h/r-CRH	17.3
1	[D-Phe^12, Aib^14]CRH	226
2	[D-Phe^12, Aib^15]CRH	8.4
3	[D-Phe^12, Cys(Et)^21]CRH	28.5
4	[D-Phe^12, Cys(Pr)^38]CRH	35
5	[D-Phe^12, Cys(Et)^21, Cys(Pr)^38]CRH	7.0
6	[D-Phe^12, Cys(Pr)^21, Cys(Et)^38]CRH	3.4
7	[D-Phe^12, Cys(Pr)^21, Cys(Pr)^38]CRH	17.3

^aThe values given are averages from 3 experiments performed in duplicates.