Target Validation Information
TTD ID	T16633
Target Name	Somatostatin receptor type 1 (SSTR1)
Type of Target	Successful
Drug Potency against Target	CAP-232	Drug Info	IC50 = 0.1 nM
	Cytotoxin Peptide Conjugate	Drug Info	IC50 = 2.79 nM	[1]
	Des-AA1,2,4,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 59 nM	[3]
	Des-AA1,2,4,13-[D-Trp8]SRIF	Drug Info	IC50 = 112 nM	[3]
	Des-AA1,2,4,5,13-[D-Trp8]-SRIF	Drug Info	IC50 = 197 nM	[3]
	Des-AA1,2,4,5-[D-Trp8]SRIF	Drug Info	IC50 = 79 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF	Drug Info	IC50 = 189 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 5.3 nM	[3]
	Des-AA1,2,5-[(NalphaMe)Cys3,D-Nal8,IAmp9]SRIF	Drug Info	IC50 = 113 nM	[2]
	Des-AA1,2,5-[(NalphaMe)Cys3,D-Trp8,IAmp9]SRIF	Drug Info	IC50 = 14 nM	[2]
	Des-AA1,2,5-[(NalphaMe)D-Nal8,IAmp9]SRIF	Drug Info	IC50 = 325 nM	[2]
	Des-AA1,2,5-[(NalphaMe)Lys4,D-Nal8,IAmp9]SRIF	Drug Info	IC50 = 535 nM	[2]
	Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9,Tyr11]SRIF	Drug Info	IC50 = 25 nM	[2]
	Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9]SRIF	Drug Info	IC50 = 69 nM	[2]
	Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Cys14]SRIF	Drug Info	IC50 = 260 nM	[2]
	Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Phe11]SRIF	Drug Info	IC50 = 583 nM	[2]
	Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Ser13]SRIF	Drug Info	IC50 = 71 nM	[2]
	Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF	Drug Info	IC50 = 176 nM	[2]
	Des-AA1,2,5-[D-Nal8,IAmp9]SRIF	Drug Info	IC50 = 248 nM	[2]
	Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9,Tyr11]SRIF	Drug Info	IC50 = 7.2 nM	[2]
	Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF	Drug Info	IC50 = 10 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Cys14]SRIF	Drug Info	IC50 = 151 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Ser13]SRIF	Drug Info	IC50 = 23 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Thr12]SRIF	Drug Info	IC50 = 75 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF	Drug Info	IC50 = 2.5 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9,Tyr11]Cbm-SRIF	Drug Info	IC50 = 8 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275	Drug Info	IC50 = 33 nM	[2]
	Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	Drug Info	IC50 = 10 nM	[2]
	Des-AA1,2,5-[IAmp9,Tyr11]-SRIF	Drug Info	IC50 = 15 nM	[2]
	Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF	Drug Info	IC50 = 720 nM	[3]
	Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF	Drug Info	IC50 = 45 nM	[2]
	Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF	Drug Info	IC50 = 16 nM	[2]
	Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF	Drug Info	IC50 = 15 nM	[2]
	Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF CH-288	Drug Info	IC50 = 14 nM	[3]
	Des-AA5-[D-Trp8]SRIF	Drug Info	IC50 = 0.98 nM	[2]
	ODT-8	Drug Info	IC50 = 27 nM	[3]
	SOMATOSTATIN	Drug Info	Ki = 2.3 nM	[4]
	SRIF-28	Drug Info	IC50 = 2.3 nM	[5]
References
REF 1	An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.
REF 2	Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem. 2005 Jan 27;48(2):507-14.
REF 3	Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22.
REF 4	Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from ... J Med Chem. 2005 Oct 20;48(21):6643-52.
REF 5	Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. J Med Chem. 2010 Aug 26;53(16):6188-97.

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