Target Validation Information
Target ID T13644
Target Name Somatostatin receptor type 3
Target Type
Successful
Drug Potency against Target Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF Drug Info IC50 = 617 nM [527384]
SRIF-28 Drug Info IC50 = 3.6 nM [531062]
Des-AA5-[D-Trp8]SRIF Drug Info IC50 = 3.4 nM [527384]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info IC50 = 222 nM [527385]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info IC50 = 39 nM [527385]
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275 Drug Info IC50 = 345 nM [527384]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF Drug Info IC50 = 500 nM [527384]
ODT-8 Drug Info IC50 = 13 nM [527385]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info IC50 = 1029 nM [527384]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info IC50 = 11 nM [527385]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info IC50 = 189 nM [527385]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 Drug Info IC50 = 543 nM [528320]
Edotreotide Drug Info IC50 = 880 nM [527508]
CytotoxinPeptide Conjugate Drug Info IC50 = 2.79 nM [526564]
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF Drug Info IC50 = 445 nM [527385]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF Drug Info IC50 = 789 nM [527385]
Des-AA1,2,4,5,10,12,13-[D-Trp8]SRIF Drug Info IC50 = 905 nM [527385]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info IC50 = 52 nM [527385]
SOMATOSTATIN Drug Info IC50 = 0.4 nM [527802]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 Drug Info IC50 = 38 nM [528320]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info IC50 = 8 nM [527384]
References
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 531062J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Ref 527508J Med Chem. 2005 Apr 21;48(8):2778-89.N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo.
Ref 526564Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527385J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Ref 527802J Med Chem. 2005 Oct 20;48(21):6643-52.Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitarycells.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
Ref 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.

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