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 | |||||
Ref 531062 | J Med Chem. 2010 Aug 26;53(16):6188-97.Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527802 | J 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 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. | ||||
Ref 526564 | Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.An adjustable release rate linking strategy for cytotoxin-peptide conjugates. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527385 | J Med Chem. 2005 Jan 27;48(2):515-22.Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. | ||||
Ref 527384 | J Med Chem. 2005 Jan 27;48(2):507-14.Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. |
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