General Information of Drug (ID: DMD42MN)

Drug Name
PF-3274167 Drug Info
Synonyms
PF-3274167; Cligosiban; 900510-03-4; UNII-D361S17AIF; D361S17AIF; CHEMBL594828; 5-(3-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridine; Cligosiban [INN]; 5-{3-[3-(2-chloro-4-fluorophenoxy)azetidin-1-yl]-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl}-2-methoxypyridine; SCHEMBL4126605; EX-A297; MolPort-044-567-557; BCP08878; ZINC38239529; BDBM50305506; AKOS030526977; CS-5337; HY-15023; PF3274167; B5924; PF 3274167; J-690387; Pyridine, 5-(3-(3-(2-chloro-4-fluorophenoxy)-1-azetidinyl)-5
Indication
Disease Entry ICD 11 Status REF
Female sexual arousal dysfunction HA01.1 Discontinued in Phase 1 [1]
Cross-matching ID
PubChem CID
11683187
CAS Number
CAS 900510-03-4
TTD Drug ID
DMD42MN

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Desmopressin DMS3GVE Diabetic complication 5A2Y Approved [3]
Mozavaptan DMZ905C Hyponatraemia 5C72 Approved [4]
Oxytocin DMDL27I Autism spectrum disorder 6A02 Approved [5]
Conivaptan DM1V329 Euvolemic hyponatremia 5C72 Approved [6]
Felypressin DMHLP9C Localisation N.A. Approved [7]
Terlipressin DMT9FH3 Hypertension BA00-BA04 Approved [8]
ATOSIBAN DMB7WYM N. A. N. A. Phase 4 [9]
Balovaptan DMKMTDG Autism spectrum disorder 6A02 Phase 3 [10]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [11]
SSR149415 DMCMD93 Anxiety disorder 6B00-6B0Z Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Oxytocin receptor (OTR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Desmopressin DMS3GVE Diabetic complication 5A2Y Approved [3]
Oxytocin DMDL27I Autism spectrum disorder 6A02 Approved [13]
Carbetocin DMUSLW3 Postpartum haemorrhage JA43 Approved [7]
ATOSIBAN DMB7WYM N. A. N. A. Phase 4 [14]
Retosiban DMOYGZF Preterm labour JB00 Phase 3 [15]
SSR149415 DMCMD93 Anxiety disorder 6B00-6B0Z Phase 2 [12]
Barusiban DMWI0X3 Androgen deficiency 5A81.1 Phase 2 [16]
FE-202767 DMDGZ1C Erectile dysfunction HA01.1 Phase 2 [13]
GSK-557296 DM3ZL2O Premature ejaculation HA03.0Z Phase 2 [17]
Pyrrolidine derivative 13 DM3VA8P N. A. N. A. Patented [18]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Oxytocin receptor (OTR) TTSCIUP OXYR_HUMAN Inhibitor [2]
Vasopressin V1a receptor (V1AR) TT4TFGN V1AR_HUMAN Inhibitor [2]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025596)
2 Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38.
3 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.
4 Nonpeptide vasopressin antagonists: a new group of hormone blockers entering the scene. Exp Clin Endocrinol Diabetes. 1999;107(3):157-65.
5 Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist. J Biol Chem. 1997 Oct 17;272(42):26536-44.
6 Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation. 2001 Nov 13;104(20):2417-23.
7 Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res. 2008;170:473-512.
8 Investigational vasopressin receptor modulators in the pipeline. Expert Opin Investig Drugs. 2009 Aug;18(8):1119-31.
9 The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
10 Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder. J Med Chem. 2020 Feb 27;63(4):1511-1525.
11 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.
12 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
13 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 369).
14 Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists. Bioorg Med Chem Lett. 2006 Feb 15;16(4):954-9.
15 The Effect of an Oxytocin Receptor Antagonist (Retosiban, GSK221149A) on the Response of Human Myometrial Explants to Prolonged Mechanical Stretch.Endocrinology.2015 Oct;156(10):3511-6.
16 The effect of barusiban, a selective oxytocin antagonist, in threatened preterm labor at late gestational age: a randomized, double-blind, placebo-controlled trial. Am J Obstet Gynecol. 2009 Jun;200(6):627.e1-10.
17 Inhibition of ejaculation by the non-peptide oxytocin receptor antagonist GSK557296: a multi-level site of action. Br J Pharmacol. 2013 Aug;169(7):1477-85.
18 A patent review of oxytocin receptor antagonists 2013-2017.Expert Opin Ther Pat. 2017 Dec;27(12):1287-1290.