Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T84486 Target Info
Target Name Oxytocin receptor (OTR)
Synonyms
OT-R
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Target Type Successful Target
Gene Name OXTR
Biochemical Class GPCR rhodopsin
UniProt ID
OXYR_HUMAN
Co-Targets of This Target  Top
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) ATOSIBAN Drug Info Ki = 0.15 nM Click to Show More [1]
2 Oxytocin Drug Info EC50 = 0.18 nM [2]
3 Carbetocin Drug Info EC50 = 2.3 nM [5]
4 SSR149415 Drug Info Ki = 22 nM [4]
5 Drug Info Ki = 62.4 nM [6]
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 [2]
2 SSR149415 Drug Info Ki = 0.6 nM [4]
3 Carbetocin Drug Info EC50 = 4.8 nM [5]
4 Drug Info Ki = 5.8 nM [6]
5 ATOSIBAN Drug Info Ki = 44 nM [1]
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) Drug Info EC50 = 0.2 nM Click to Show More [3]
2 Oxytocin Drug Info EC50 = 7.3 nM [7]
3 Carbetocin Drug Info EC50 = 170 nM [7]
4 SSR149415 Drug Info Ki = 290 nM [8]
5 ATOSIBAN Drug Info Ki = 330 nM [1]
6 Retosiban Drug Info Ki = 950 nM [1]
References  Top
REF 1 The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
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 Discovery of Potent, Selective, and Short-Acting Peptidic V 2 Receptor Agonists. J Med Chem. 2019 May 23;62(10):4991-5005.
REF 4 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
REF 5 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 6 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 7 New, potent, and selective peptidic oxytocin receptor agonists. J Med Chem. 2014 Jun 26;57(12):5306-17.
REF 8 Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3828-31.

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