Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T79232 | Target Info | |||
| Target Name | Vasopressin V1a receptor (V1AR) | ||||
| Synonyms |
Vascular/hepatic-type arginine vasopressin receptor; V1aR; V1a vasopressin receptor; Antidiuretic hormone receptor 1a; AVPR1; AVPR V1a
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| Target Type | Successful Target | ||||
| Gene Name | AVPR1A | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Oxytocin receptor (OTR) | Successful Target | ||||
| UniProt ID | OXYR_HUMAN | |||||
| Gene Name | OXTR | |||||
| Synonyms |
OT-R
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| Representative Drug(s) | Oxytocin | Drug Info | EC50 = 0.0046 nM | Click to Show More | [1] | |
| 2 | SSR149415 | Drug Info | Ki = 1.514 nM | [5] | ||
| 3 | FE-202158 | Drug Info | EC50 = 2.399 nM | [6] | ||
| 4 | ATOSIBAN | Drug Info | Ki = 11 nM | [10] | ||
| 5 | Desmopressin | Drug Info | EC50 = 72 nM | [8] | ||
| 6 | Mozavaptan | Drug Info | Ki = 660 nM | [13] | ||
| Co-Target Name | Vasopressin V1b receptor (V1BR) | Successful Target | ||||
| UniProt ID | V1BR_HUMAN | |||||
| Gene Name | AVPR1B | |||||
| Synonyms |
Vasopressin V3 receptor; Vasopressin V(1b) Receptor; VPR3; V1bR; Antidiuretic hormone receptor 1b; AVPR3; AVPR V3; AVPR V1b
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| Representative Drug(s) | Oxytocin | Drug Info | EC50 = 0.2 nM | Click to Show More | [1] | |
| 2 | SSR149415 | Drug Info | Ki = 0.6 nM | [4] | ||
| 3 | Desmopressin | Drug Info | Ki = 5.8 nM | [7] | ||
| 4 | ATOSIBAN | Drug Info | Ki = 44 nM | [10] | ||
| 5 | FE-202158 | Drug Info | EC50 = 338.84 nM | [6] | ||
| Co-Target Name | Vasopressin V2 receptor (V2R) | Successful Target | ||||
| UniProt ID | V2R_HUMAN | |||||
| Gene Name | AVPR2 | |||||
| Synonyms |
Renal-type arginine vasopressin receptor; DIR3; DIR; Antidiuretic hormone receptor; AVPR V2; ADHR
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| Representative Drug(s) | Desmopressin | Drug Info | EC50 = 0.2 nM | Click to Show More | [2] | |
| 2 | Conivaptan | Drug Info | Ki = 0.36 nM | [3] | ||
| 3 | Oxytocin | Drug Info | EC50 = 7.3 nM | [8] | ||
| 4 | Mozavaptan | Drug Info | Ki = 9.42 nM | [9] | ||
| 5 | SSR149415 | Drug Info | Ki = 290 nM | [11] | ||
| 6 | ATOSIBAN | Drug Info | Ki = 330 nM | [10] | ||
| Co-Target Name | Melanocortin receptor 4 (MC4R) | Successful Target | ||||
| UniProt ID | MC4R_HUMAN | |||||
| Gene Name | MC4R | |||||
| Synonyms |
MC4-R
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| Representative Drug(s) | PMX-53 | Drug Info | IC50 = 400 nM | [12] | ||
| Co-Target Name | C5a anaphylatoxin chemotactic receptor (C5AR1) | Successful Target | ||||
| UniProt ID | C5AR1_HUMAN | |||||
| Gene Name | C5AR1 | |||||
| Synonyms |
CD88; C5aR; C5a-R; C5a anaphylatoxin chemotactic receptor 1; C5R1
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| Representative Drug(s) | PMX-53 | Drug Info | IC50 = 15 nM | [14] | ||
| Co-Target Name | Substance-K receptor (TACR2) | Clinical trial Target | ||||
| UniProt ID | NK2R_HUMAN | |||||
| Gene Name | TACR2 | |||||
| Synonyms |
Tachykinin receptor 2; Tachykinin neurokinin 2 receptor; TACR2; SKR; Neurokinin A receptor; NK-2R; NK-2 receptor
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| Representative Drug(s) | PMX-53 | Drug Info | IC50 = 87 nM | [12] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis of oxytocin derivatives lipidated via a carbonate or carbamate linkage as a long-acting therapeutic agent for social impairment-like behaviors. Bioorg Med Chem. 2019 Aug 1;27(15):3358-3363. | ||||
| REF 2 | Discovery of Potent, Selective, and Short-Acting Peptidic V 2 Receptor Agonists. J Med Chem. 2019 May 23;62(10):4991-5005. | ||||
| REF 3 | Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3742-5. | ||||
| REF 4 | Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. | ||||
| REF 5 | The characterization of a novel V1b antagonist lead series. Bioorg Med Chem Lett. 2011 Jan 1;21(1):92-6. | ||||
| REF 6 | New, potent, selective, and short-acting peptidic V1a receptor agonists. J Med Chem. 2011 Jul 14;54(13):4388-98. | ||||
| REF 7 | Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88. | ||||
| REF 8 | New, potent, and selective peptidic oxytocin receptor agonists. J Med Chem. 2014 Jun 26;57(12):5306-17. | ||||
| REF 9 | Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template. J Med Chem. 2000 Nov 16;43(23):4388-97. | ||||
| REF 10 | The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. | ||||
| REF 11 | Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3828-31. | ||||
| REF 12 | Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92. | ||||
| REF 13 | Selective fluorescent nonpeptidic antagonists for vasopressin V? GPCR: application to ligand screening and oligomerization assays. J Med Chem. 2012 Oct 25;55(20):8588-602. | ||||
| REF 14 | Selective hexapeptide agonists and antagonists for human complement C3a receptor. J Med Chem. 2010 Jul 8;53(13):4938-48. | ||||
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