Target Validation Information
Target ID T16633
Target Name Somatostatin receptor 1
Target Type
Successful
Drug Potency against Target CAP-232 Drug Info IC50 = 0.1 nM
SRIF-28 Drug Info IC50 = 2.3 nM [531062]
Des-AA1,2,4,13-[D-Trp8]SRIF Drug Info IC50 = 112 nM [527385]
Des-AA1,2,5,12,13-[D-Trp8,IAmp9]SRIF Drug Info IC50 = 189 nM [527385]
Des-AA1,2,5-[D-Trp8,IAmp9]SRIF CH-275 Drug Info IC50 = 33 nM [527384]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]Cbm-SRIF Drug Info IC50 = 15 nM [527384]
Des-AA1,2,5-[D-Trp8,IAmp9,m-I-Tyr11]Cbm-SRIF Drug Info IC50 = 2.5 nM [527384]
Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9,Tyr11]SRIF Drug Info IC50 = 25 nM [527384]
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Ser13]SRIF Drug Info IC50 = 23 nM [527384]
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Cys14]SRIF Drug Info IC50 = 151 nM [527384]
Des-AA1,2,5-[D-Nal8,(NalphaMe)IAmp9]SRIF Drug Info IC50 = 69 nM [527384]
Des-AA1,2,5-[(NalphaMe)D-Nal8,IAmp9]SRIF Drug Info IC50 = 325 nM [527384]
Des-AA1,2,5-[D-Trp8,IAmp9,(NalphaMe)Thr12]SRIF Drug Info IC50 = 75 nM [527384]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Cys14]SRIF Drug Info IC50 = 260 nM [527384]
Des-AA1,2,5-[(NalphaMe)Cys3,D-Nal8,IAmp9]SRIF Drug Info IC50 = 113 nM [527384]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Ser13]SRIF Drug Info IC50 = 71 nM [527384]
Des-AA1,2,5-[(NalphaMe)Cys3,D-Trp8,IAmp9]SRIF Drug Info IC50 = 14 nM [527384]
Des-AA1,2,5-[D-Trp8,IAmp9,Tyr11]Cbm-SRIF Drug Info IC50 = 8 nM [527384]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Thr12]SRIF Drug Info IC50 = 176 nM [527384]
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF CH-288 Drug Info IC50 = 14 nM [527385]
Des-AA1,2,5,12,13-[D-Trp8]SRIF Drug Info IC50 = 5.3 nM [527385]
Des-AA1,2,4,12,13-[D-Trp8]SRIF Drug Info IC50 = 59 nM [527385]
Des-AA1,4,5,13-[Tyr2,D-Trp8]-SRIF Drug Info IC50 = 720 nM [527385]
Des-AA1,2,5-[D-Nal8,IAmp9]SRIF Drug Info IC50 = 248 nM [527384]
Des-AA1,2,5-[D-Nal8,IAmp9,(NalphaMe)Phe11]SRIF Drug Info IC50 = 583 nM [527384]
SOMATOSTATIN Drug Info Ki = 2.3 nM [527802]
Des-AA5-[D-Trp8]SRIF Drug Info IC50 = 0.98 nM [527384]
Des-AA1,2,4,5,13-[D-Trp8]-SRIF Drug Info IC50 = 197 nM [527385]
Des-AA1,2,5-[IAmp9,Tyr11]-SRIF Drug Info IC50 = 15 nM [527384]
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]Cbm-SRIF Drug Info IC50 = 45 nM [527384]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF Drug Info IC50 = 10 nM [527384]
Des-AA1,2,5-[(NalphaMe)Lys4,D-Nal8,IAmp9]SRIF Drug Info IC50 = 535 nM [527384]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info IC50 = 10 nM [527384]
Des-AA1,5-[Tyr2,D-Trp8,(NalphaMe)IAmp9]SRIF Drug Info IC50 = 16 nM [527384]
CytotoxinPeptide Conjugate Drug Info IC50 = 2.79 nM [526564]
Des-AA1,2,4,5-[D-Trp8]SRIF Drug Info IC50 = 79 nM [527385]
ODT-8 Drug Info IC50 = 27 nM [527385]
Des-AA1,2,5-[D-Trp8,(NalphaMe)IAmp9,Tyr11]SRIF Drug Info IC50 = 7.2 nM [527384]
The Effect of Target Knockout, Knockdown or Genetic Variations In the retina of wild type (WT) mice, sst1 receptors are localised to somatostatin-14(SRIF)-containing amacrine cells, whereas in the retina of sst1 KO mice, sst1 receptors are absent. sst1 receptor loss causes a significant increase in retinal levels of SRIF, whereas it does not affect SRIF messenger RNA indicating that sst1 receptors play a role in limiting retinal SRIF atthe post-transcriptional level. As another consequence of sst1 receptor loss, levels of expression of sst2 receptors are significantly higher than in control retinas. Together, these findings providethe first demonstration of prominent compensatory regulation in the mouse retina as a consequence of a distinct SRIF receptor deletion. The fact that in the absence of the sst1 receptor, retinal SRIFincreases in concomitance with an increase in sst2 receptors suggests that SRIF may regulate sst2 receptor expression and that this regulatory process is controlled upstream by the sst1 receptor. This finding can be important in the design of drugs affecting SRIF function, not only in the retina, but also elsewhere in the brain
References
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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 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 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 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 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 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 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 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 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 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 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 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 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 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
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 527384J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.

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