Target Validation Information
TTD ID	T13644
Target Name	Somatostatin receptor type 3 (SSTR3)
Type of Target	Successful
Drug Potency against Target	Cytotoxin Peptide Conjugate	Drug Info	IC50 = 2.79 nM	[1]
	Des-AA1,2,4,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 189 nM	[3]
	Des-AA1,2,4,13-[D-Trp8]SRIF	Drug Info	IC50 = 11 nM	[3]
	Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 905 nM	[3]
	Des-AA1,2,4,5,13-[D-Trp8]-SRIF	Drug Info	IC50 = 52 nM	[3]
	Des-AA1,2,4,5-[D-Trp8]SRIF	Drug Info	IC50 = 222 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF	Drug Info	IC50 = 789 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 39 nM	[3]
	Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF	Drug Info	IC50 = 1029 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF	Drug Info	IC50 = 617 nM	[2]
	Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275	Drug Info	IC50 = 345 nM	[2]
	Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	Drug Info	IC50 = 8 nM	[2]
	Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF	Drug Info	IC50 = 445 nM	[3]
	Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF	Drug Info	IC50 = 500 nM	[2]
	Des-AA5-[D-Trp8]SRIF	Drug Info	IC50 = 3.4 nM	[2]
	Edotreotide	Drug Info	IC50 = 880 nM	[4]
	H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2	Drug Info	IC50 = 543 nM	[6]
	H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2	Drug Info	IC50 = 38 nM	[6]
	ODT-8	Drug Info	IC50 = 13 nM	[3]
	SOMATOSTATIN	Drug Info	IC50 = 0.4 nM	[5]
	SRIF-28	Drug Info	IC50 = 3.6 nM	[7]
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	N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vi... J Med Chem. 2005 Apr 21;48(8):2778-89.
REF 5	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 6	Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. J Med Chem. 2006 Jul 27;49(15):4487-96.
REF 7	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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