Target Validation Information
TTD ID	T53024
Target Name	Somatostatin receptor type 2 (SSTR2)
Type of Target	Successful
Drug Potency against Target	BIM23A760	Drug Info	IC50 = 18.3 nM	[9]
	Ala11-SRIF-14-amide	Drug Info	Ki = 6.3 nM	[5]
	Ala6-SRIF-14-amide	Drug Info	Ki = 20 nM	[5]
	Ala7-SRIF-14-amide	Drug Info	Ki = 20 nM	[5]
	Cytotoxin Peptide Conjugate	Drug Info	IC50 = 2.79 nM	[1]
	D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2	Drug Info	IC50 = 18.6 nM	[6]
	Des-AA1,2,4,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 95 nM	[3]
	Des-AA1,2,4,13-[D-Trp8]SRIF	Drug Info	IC50 = 5 nM	[3]
	Des-AA1,2,4,5,11,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 598 nM	[3]
	Des-AA1,2,4,5,13-[D-Trp8]-SRIF	Drug Info	IC50 = 1.9 nM	[3]
	Des-AA1,2,4,5,6,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 531 nM	[3]
	Des-AA1,2,4,5-[D-Trp8]SRIF	Drug Info	IC50 = 28 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 15 nM	[3]
	Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	Drug Info	IC50 = 16 nM	[2]
	Des-AA5-[D-Trp8]SRIF	Drug Info	IC50 = 43 nM	[2]
	Edotreotide	Drug Info	IC50 = 14 nM	[4]
	H-c[Cys-Phe-DTrp-Lys-Thr-Cys]-OH	Drug Info	IC50 = 378 nM	[7]
	H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2	Drug Info	Ki = 1.7 nM	[6]
	H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2	Drug Info	IC50 = 3.6 nM	[7]
	H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2	Drug Info	IC50 = 2.2 nM	[7]
	ODT-8	Drug Info	IC50 = 41 nM	[3]
	Pyz11-D-Trp8-SRIF	Drug Info	Ki = 1 nM	[5]
	Pyz6-D-Trp8-SRIF	Drug Info	Ki = 7 nM	[5]
	SOMATOSTATIN	Drug Info	Ki = 0.23 nM	[6]
	SRIF-28	Drug Info	IC50 = 3 nM	[8]
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	Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSS... J Med Chem. 2005 Jun 16;48(12):4025-30.
REF 6	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 7	Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. J Med Chem. 2006 Jul 27;49(15):4487-96.
REF 8	Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. J Med Chem. 2010 Aug 26;53(16):6188-97.
REF 9	Differential cytotoxicity of novel somatostatin and dopamine chimeric compounds on bronchopulmonary and small intestinal neuroendocrine tumor cell lines. Cancer. 2008 Aug 15;113(4):690-700.

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