Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T53024 | Target Info | |||
| Target Name | Somatostatin receptor type 2 (SSTR2) | ||||
| Synonyms |
Sst(2); Somatostatin receptor 2; SS2R; SS2-R; SS-2-R; SRIF-1
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| Target Type | Successful Target | ||||
| Gene Name | SSTR2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Somatostatin receptor type 5 (SSTR5) | Successful Target | ||||
| UniProt ID | SSR5_HUMAN | |||||
| Gene Name | SSTR5 | |||||
| Synonyms |
Somatostatin receptor 5; SSTR5; SS5R
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| Representative Drug(s) | Pasireotide | Drug Info | Ki = 0.1259 nM | Click to Show More | [1] | |
| 2 | ODT-8 | Drug Info | IC50 = 2.6 nM | [2] | ||
| 3 | Octreotide | Drug Info | IC50 = 22 nM | [3] | ||
| Co-Target Name | Somatostatin receptor type 3 (SSTR3) | Successful Target | ||||
| UniProt ID | SSR3_HUMAN | |||||
| Gene Name | SSTR3 | |||||
| Synonyms |
SSTR3; SSR-28; SS3R
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| Representative Drug(s) | Pasireotide | Drug Info | Ki = 0.7943 nM | Click to Show More | [1] | |
| 2 | ODT-8 | Drug Info | EC50 = 3.33 nM | [2] | ||
| Co-Target Name | Somatostatin receptor type 1 (SSTR1) | Successful Target | ||||
| UniProt ID | SSR1_HUMAN | |||||
| Gene Name | SSTR1 | |||||
| Synonyms |
Sst(1); Somatostatin receptor 1; SSTR1; SS1R; SRIF-2
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| Representative Drug(s) | Pasireotide | Drug Info | Ki = 6.31 nM | Click to Show More | [1] | |
| 2 | ODT-8 | Drug Info | IC50 = 27 nM | [2] | ||
| Co-Target Name | Somatostatin receptor type 4 (SSTR4) | Clinical trial Target | ||||
| UniProt ID | SSR4_HUMAN | |||||
| Gene Name | SSTR4 | |||||
| Synonyms |
SSTR4; SS4R
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| Representative Drug(s) | ODT-8 | Drug Info | IC50 = 1.8 nM | Click to Show More | [4] | |
| 2 | Octreotide | Drug Info | Ki = 66 nM | [5] | ||
| 3 | Pasireotide | Drug Info | Ki < 100 nM | [1] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem. 2003 Jun 5;46(12):2334-44. | ||||
| REF 2 | N-imidazolebenzyl-histidine substitution in somatostatin and in its octapeptide analogue modulates receptor selectivity and function. J Med Chem. 2011 Sep 8;54(17):5981-7. | ||||
| REF 3 | Ligand design for somatostatin receptor isoforms 4 and 5. Eur J Med Chem. 2019 Feb 1;163:148-159. | ||||
| REF 4 | Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling. J Med Chem. 2003 Dec 18;46(26):5597-605. | ||||
| REF 5 | Discovery of a 3,4,5-trisubstituted-1,2,4-triazole agonist with high affinity and selectivity at the somatostatin subtype-4 (sst4) receptor. Med. Chem. Commun. 2018;9: 2083-2090. | ||||
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