Table 1

Screening of a combinatorial synthetic peptide library using the yeast SRIF antagonist bioassay

Sample type	AA₁	AA₂	AA₃	AA₄	AA₅	AA₆	Zone
							mm
Library	His	Tyr	Ran	Ran	Ran	Ran	12.5
	His	Trp	Ran	Ran	Ran	Ran	12
	His	Phe	Ran	Ran	Ran	Ran	13
	Trp	Tyr	Ran	Ran	Ran	Ran	12.5
	Phe	His	Ran	Ran	Ran	Ran	13.5
BIM-23066a							19.5
1st iteration	His	Phe	Ran	Ran	Ran	Ran	5
	His	Phe	Cys	Ran	Ran	Ran	9
	His	Phe	Val	Ran	Ran	Ran	9.5
	His	Phe	Leu	Ran	Ran	Ran	7
	His	Phe	Thr	Ran	Ran	Ran	7
	His	Phe	Ile	Ran	Ran	Ran	10
	His	Phe	Trp	Ran	Ran	Ran	7
BIM-23066a							13
2nd iteration	His	Phe	Ile	Ran	Ran	Ran	11
	His	Phe	Ile	His	Ran	Ran	11
	His	Phe	Ile	Pro	Ran	Ran	11.5
	His	Phe	Ile	Arg	Ran	Ran	12.5
	His	Phe	Ile	Asn	Ran	Ran	11
	His	Phe	Ile	Trp	Ran	Ran	11
	His	Phe	Ile	Lys	Ran	Ran	12.5
BIM-23066a							11
3rd iteration	His	Phe	Ile	Arg	Ran	Ran	15
	His	Phe	Ile	Arg	His	Ran	12
	His	Phe	Ile	Arg	Leu	Ran	12
	His	Phe	Ile	Arg	Arg	Ran	13
	His	Phe	Ile	Arg	Tyr	Ran	15
	His	Phe	Ile	Arg	Ile	Ran	12
	His	Phe	Ile	Arg	Met	Ran	13
	His	Phe	Ile	Arg	Trp	Ran	23
	His	Phe	Ile	Arg	Gly	Ran	18
BIM-23066a							13
4th iteration	His	Phe	Ile	Arg	Trp	Ran	15
	His	Phe	Ile	Arg	Trp	Leu	15
	His	Phe	Ile	Arg	Trp	Thr	14
	His	Phe	Ile	Arg	Trp	Tyr	16
	His	Phe	Ile	Arg	Trp	Ile	16
	His	Phe	Ile	Arg	Trp	Ala	15
	His	Phe	Ile	Arg	Trp	Asn	15
	His	Phe	Ile	Arg	Trp	Met	18
	His	Phe	Ile	Arg	Trp	Trp	16
	His	Phe	Ile	Arg	Trp	Phe	18
	His	Phe	Ile	Arg	Trp	Gly	13
	His	Phe	Ile	Arg	Trp	Gln	16

Samples in bold type were chosen for further synthesis. Boxed regions of the table denote individual assays. BIM-23066a was tested at 1 mm in DMSO. Ran, random; zone, inhibition zone.