Target Validation Information
TTD ID	T62974
Target Name	Somatostatin receptor type 4 (SSTR4)
Type of Target	Clinical trial
Drug Potency against Target	CAP-232	Drug Info	IC50 = 0.1 nM
	Ala11-SRIF-14-amide	Drug Info	Ki < 1 nM	[4]
	Ala6-SRIF-14-amide	Drug Info	Ki = 80 nM	[4]
	Cytotoxin Peptide Conjugate	Drug Info	IC50 = 2.79 nM	[1]
	D-Trp8-SRIF-14	Drug Info	Ki = 3.7 nM	[4]
	Des-AA1,2,4,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 1.2 nM	[3]
	Des-AA1,2,4,13-[D-Trp8]SRIF	Drug Info	IC50 = 1.4 nM	[3]
	Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 786 nM	[3]
	Des-AA1,2,4,5,13-[D-Trp8]-SRIF	Drug Info	IC50 = 1 nM	[3]
	Des-AA1,2,4,5,6,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 229 nM	[3]
	Des-AA1,2,4,5-[D-Trp8]SRIF	Drug Info	IC50 = 3.3 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF	Drug Info	IC50 = 932 nM	[3]
	Des-AA1,2,5,12,13-[D-Trp8]SRIF	Drug Info	IC50 = 0.6 nM	[3]
	Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF	Drug Info	IC50 = 417 nM	[2]
	Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF	Drug Info	IC50 = 226 nM	[2]
	Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	Drug Info	IC50 = 0.5 nM	[2]
	Des-AA1,2,5-[IAmp9,Tyr11]-SRIF	Drug Info	IC50 = 384 nM	[2]
	Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF	Drug Info	IC50 = 418 nM	[2]
	Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF	Drug Info	IC50 = 245 nM	[2]
	Des-AA5-[D-Trp8]SRIF	Drug Info	IC50 = 1.7 nM	[2]
	ODT-8	Drug Info	IC50 = 1.8 nM	[3]
	Pyz11-D-Trp8-SRIF	Drug Info	Ki = 124 nM	[4]
	Pyz6-D-Trp8-SRIF	Drug Info	Ki = 77 nM	[4]
	Pyz7-D-Trp8-SRIF	Drug Info	Ki = 700 nM	[4]
	SOMATOSTATIN	Drug Info	Ki = 1.7 nM	[5]
	SRIF-28	Drug Info	IC50 = 1.6 nM	[7]
Action against Disease Model	TLN-4601	Drug Info	TLN-4601 potently inhibited the anchorage-dependent and -independent growth of KRAS-transformed h uMan nestin-positive (HPNE) pancreatic duct-derived cells. The growth of KRAS mutation-positive pancreatic carcinoma cell lines (PDAC) was inhibited by TLN-4601.	[6]
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	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 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	Identification, characterization and potent antitumor activity of ECO-4601, a novel peripheral benzodiazepine receptor ligand. Cancer Chemother Pharmacol. 2008 May;61(6):911-21.
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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