Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T66237 Target Info
Target Name Vasopressin V2 receptor (V2R)
Synonyms
Renal-type arginine vasopressin receptor; DIR3; DIR; Antidiuretic hormone receptor; AVPR V2; ADHR
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Target Type Successful Target
Gene Name AVPR2
Biochemical Class GPCR rhodopsin
UniProt ID
V2R_HUMAN
Co-Targets of This Target  Top
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) Vasopressin Drug Info EC50 = 0.0035 nM Click to Show More [1]
2 Oxytocin Drug Info EC50 = 0.2 nM [2]
3 SSR149415 Drug Info Ki = 0.6 nM [5]
4 Drug Info Ki = 5.8 nM [7]
5 ATOSIBAN Drug Info Ki = 44 nM [3]
Co-Target Name Vasopressin V1a receptor (V1AR) Successful Target
UniProt ID V1AR_HUMAN
Gene Name AVPR1A
Synonyms
Vascular/hepatic-type arginine vasopressin receptor; V1aR; V1a vasopressin receptor; Antidiuretic hormone receptor 1a; AVPR1; AVPR V1a
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Representative Drug(s) Vasopressin Drug Info EC50 = 0.004 nM Click to Show More [1]
2 ATOSIBAN Drug Info Ki = 0.15 nM [3]
3 Oxytocin Drug Info EC50 = 0.18 nM [2]
4 Drug Info Ki = 0.43 nM [4]
5 SSR149415 Drug Info Ki = 22 nM [5]
6 Lixivaptan Drug Info Ki = 44 nM [8]
7 Drug Info Ki = 62.4 nM [7]
8 Mozavaptan Drug Info Ki = 195 nM [10]
9 Satavaptan Drug Info Ki = 304 nM [11]
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 [2]
2 Vasopressin Drug Info EC50 = 0.1 nM [1]
3 SSR149415 Drug Info Ki = 1.514 nM [6]
4 ATOSIBAN Drug Info Ki = 11 nM [3]
5 Drug Info EC50 = 72 nM [9]
6 Lixivaptan Drug Info IC50 = 519 nM [12]
7 Mozavaptan Drug Info Ki = 660 nM [10]
References  Top
REF 1 Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors. J Med Chem. 2019 Apr 11;62(7):3297-3310.
REF 2 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 3 The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
REF 4 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 5 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
REF 6 The characterization of a novel V1b antagonist lead series. Bioorg Med Chem Lett. 2011 Jan 1;21(1):92-6.
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 Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2747-52.
REF 9 New, potent, and selective peptidic oxytocin receptor agonists. J Med Chem. 2014 Jun 26;57(12):5306-17.
REF 10 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 11 Receptor-Ligand Interaction Measured by Inductively Coupled Plasma Mass Spectrometry and Selenium Labeling. J Med Chem. 2018 Nov 21;61(22):10173-84.
REF 12 Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5796-800.

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