Target Validation Information
Target ID T53024
Target Name Somatostatin receptor type 2
Target Type
Successful
Drug Potency against Target SRIF-28 Drug Info IC50 = 3 nM [531062]
H-D-Phe-c[Cys-Ala-D-Trp-Lys-Thr-Cys]-Thr-NH2 Drug Info IC50 = 3.6 nM [528320]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info IC50 = 28 nM [527385]
Des-AA5-[D-Trp8]SRIF Drug Info IC50 = 43 nM [527384]
Pyz11-D-Trp8-SRIF Drug Info Ki = 1 nM [527585]
H-c[Cys-Phe-DTrp-Lys-Thr-Cys]-OH Drug Info IC50 = 378 nM [528320]
Des-AA1,2,4,5,6,12,13-[D-Trp8]SRIF Drug Info IC50 = 531 nM [527385]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info IC50 = 1.9 nM [527385]
BIM23A760 Drug Info IC50 = 18.3 nM [552837]
H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 Drug Info Ki = 1.7 nM [527802]
CytotoxinPeptide Conjugate Drug Info IC50 = 2.79 nM [526564]
Pyz6-D-Trp8-SRIF Drug Info Ki = 7 nM [527585]
Ala6-SRIF-14-amide Drug Info Ki = 20 nM [527585]
Ala11-SRIF-14-amide Drug Info Ki = 6.3 nM [527585]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info IC50 = 16 nM [527384]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info IC50 = 5 nM [527385]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info IC50 = 15 nM [527385]
D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Asp-NH2 Drug Info IC50 = 18.6 nM [527802]
Ala7-SRIF-14-amide Drug Info Ki = 20 nM [527585]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info IC50 = 95 nM [527385]
Des-AA1,2,4,5,11,12,13-[D-Trp8]SRIF Drug Info IC50 = 598 nM [527385]
ODT-8 Drug Info IC50 = 41 nM [527385]
Edotreotide Drug Info IC50 = 14 nM [527508]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 Drug Info IC50 = 2.2 nM [528320]
SOMATOSTATIN Drug Info Ki = 0.23 nM [527802]
References
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 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
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 527585J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4.An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
Ref 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
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 552837Differential 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. doi: 10.1002/cncr.23700.
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 526564Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
Ref 527585J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4.An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
Ref 527585J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4.An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
Ref 527585J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4.An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
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 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 527585J Med Chem. 2005 Jun 16;48(12):4025-30.Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4.An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.
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 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 528320J Med Chem. 2006 Jul 27;49(15):4487-96.Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR.
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.

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