way-151932 profile

WAY-151932: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	5311500
CHEMBL ID	363910
SCHEMBL ID	6627050
MeSH ID	M0497375

Synonym
way-vna-932
way-151932
vna-932
vna932
CHEMBL363910 ,
bdbm50177593
(5h-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10(11h)-yl)(2-chloro-4-(3-methyl-1h-pyrazol-1-yl)phenyl)methanone
(5h,11h-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10-yl)-[2-chloro-4-(3-methyl-pyrazol-1-yl)-phenyl]-methanone
[2-chloro-4-(3-methylpyrazol-1-yl)phenyl]-(6,11-dihydropyrrolo[2,1-c][1,4]benzodiazepin-5-yl)methanone
gtpl3537
vna 932
SCHEMBL6627050
[2-chloro-4-(3-methyl-pyrazol-1-yl)-phenyl]-(5h,11h-pyrrolo-[2,1-c][1,4]benzodiazepin-10-yl)-methanone
JXKQHDZUZGKDGO-UHFFFAOYSA-N
[2-chloro-4-(3-methyl-pyrazol-1-yl)-phenyl]-(5h,11h-pyrrolo[2,1-c][1,4]benzodiazepin-10-yl)-methanone
HY-19381
CS-6661
unii-cc7iz88xd2
methanone, (2-chloro-4-(3-methyl-1h-pyrazol-1-yl)phenyl)-5h-pyrrolo(2,1-c)(1,4)benzodiazepin-10(11h)-yl-
(2-chloro-4-(3-methyl-pyrazol-1-yl)-phenyl)-(5h,11h-pyrrolo(2,1-c)benzodiazepin-10-yl)-methanone
(2-chloro-4-(3-methyl-1h-pyrazol-1-yl)phenyl)-5h-pyrrolo(2,1-c)(1,4)benzodiazepin-10(11h)-ylmethanone
220460-92-4
CC7IZ88XD2 ,
Q27089151
MS-26878
AKOS040742823

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Vasopressin V2 receptor	Homo sapiens (human)	IC50 (µMol)	0.0802	0.0000	1.1213	7.0000	AID260564; AID301764
Vasopressin V2 receptor	Homo sapiens (human)	Ki	0.0466	0.0004	0.4345	3.9811	AID1386883; AID1386910; AID458564
Oxytocin receptor	Homo sapiens (human)	IC50 (µMol)	0.3530	0.0027	0.2191	0.5190	AID301768
Oxytocin receptor	Homo sapiens (human)	Ki	0.1743	0.0001	0.0718	0.9780	AID1386901; AID1386911; AID458553
Delta-type opioid receptor	Mus musculus (house mouse)	IC50 (µMol)	0.0800	0.0001	0.7298	10.0000	AID260564
Vasopressin V1a receptor	Homo sapiens (human)	IC50 (µMol)	1.0720	0.0006	0.3835	2.0000	AID1386903; AID260560; AID301767
Vasopressin V1a receptor	Homo sapiens (human)	Ki	0.3843	0.0002	0.6235	7.0300	AID1386881; AID1386909; AID458560
Vasopressin V1b receptor	Homo sapiens (human)	Ki	1.0000	0.0005	0.1897	1.7820	AID1386882
Oxytocin receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0550	0.0089	0.2992	0.7800	AID1386904
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Vasopressin V2 receptor	Homo sapiens (human)	EC50 (µMol)	0.0106	0.0000	0.5506	6.7000	AID1386902; AID260559; AID412970; AID458577
Oxytocin receptor	Homo sapiens (human)	EC50 (µMol)	0.1250	0.0000	0.0805	0.8810	AID458559
Vasopressin V1a receptor	Homo sapiens (human)	EC50 (µMol)	0.4650	0.0000	0.1971	3.2000	AID458576
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Vasopressin V2 receptor	Homo sapiens (human)	Kact	0.0095	0.0003	0.0064	0.0095	AID1386912; AID458565
Oxytocin receptor	Homo sapiens (human)	Kinact	0.4880	0.0009	0.3256	0.4880	AID1386917; AID458556
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
positive regulation of systemic arterial blood pressure	Vasopressin V2 receptor	Homo sapiens (human)
renal water retention	Vasopressin V2 receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Vasopressin V2 receptor	Homo sapiens (human)
activation of adenylate cyclase activity	Vasopressin V2 receptor	Homo sapiens (human)
hemostasis	Vasopressin V2 receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Vasopressin V2 receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Vasopressin V2 receptor	Homo sapiens (human)
positive regulation of gene expression	Vasopressin V2 receptor	Homo sapiens (human)
telencephalon development	Vasopressin V2 receptor	Homo sapiens (human)
response to cytokine	Vasopressin V2 receptor	Homo sapiens (human)
positive regulation of intracellular signal transduction	Vasopressin V2 receptor	Homo sapiens (human)
cellular response to hormone stimulus	Vasopressin V2 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Vasopressin V2 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Vasopressin V2 receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure by vasopressin	Vasopressin V2 receptor	Homo sapiens (human)
suckling behavior	Oxytocin receptor	Homo sapiens (human)
response to amphetamine	Oxytocin receptor	Homo sapiens (human)
muscle contraction	Oxytocin receptor	Homo sapiens (human)
cell surface receptor signaling pathway	Oxytocin receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Oxytocin receptor	Homo sapiens (human)
heart development	Oxytocin receptor	Homo sapiens (human)
lactation	Oxytocin receptor	Homo sapiens (human)
memory	Oxytocin receptor	Homo sapiens (human)
response to xenobiotic stimulus	Oxytocin receptor	Homo sapiens (human)
positive regulation of norepinephrine secretion	Oxytocin receptor	Homo sapiens (human)
telencephalon development	Oxytocin receptor	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Oxytocin receptor	Homo sapiens (human)
response to estradiol	Oxytocin receptor	Homo sapiens (human)
response to progesterone	Oxytocin receptor	Homo sapiens (human)
response to anoxia	Oxytocin receptor	Homo sapiens (human)
response to cytokine	Oxytocin receptor	Homo sapiens (human)
social behavior	Oxytocin receptor	Homo sapiens (human)
response to cocaine	Oxytocin receptor	Homo sapiens (human)
maternal behavior	Oxytocin receptor	Homo sapiens (human)
sperm ejaculation	Oxytocin receptor	Homo sapiens (human)
eating behavior	Oxytocin receptor	Homo sapiens (human)
response to peptide hormone	Oxytocin receptor	Homo sapiens (human)
estrous cycle	Oxytocin receptor	Homo sapiens (human)
positive regulation of blood pressure	Oxytocin receptor	Homo sapiens (human)
digestive tract development	Oxytocin receptor	Homo sapiens (human)
positive regulation of synapse assembly	Oxytocin receptor	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Oxytocin receptor	Homo sapiens (human)
positive regulation of penile erection	Oxytocin receptor	Homo sapiens (human)
ERK1 and ERK2 cascade	Oxytocin receptor	Homo sapiens (human)
positive regulation of uterine smooth muscle contraction	Oxytocin receptor	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Oxytocin receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Oxytocin receptor	Homo sapiens (human)
female pregnancy	Oxytocin receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure by vasopressin	Oxytocin receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Oxytocin receptor	Homo sapiens (human)
maternal process involved in parturition	Oxytocin receptor	Homo sapiens (human)
cellular response to hormone stimulus	Oxytocin receptor	Homo sapiens (human)
maternal aggressive behavior	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of systemic arterial blood pressure	Vasopressin V1a receptor	Homo sapiens (human)
generation of precursor metabolites and energy	Vasopressin V1a receptor	Homo sapiens (human)
activation of phospholipase C activity	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Vasopressin V1a receptor	Homo sapiens (human)
negative regulation of female receptivity	Vasopressin V1a receptor	Homo sapiens (human)
grooming behavior	Vasopressin V1a receptor	Homo sapiens (human)
blood circulation	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of heart rate	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of glutamate secretion	Vasopressin V1a receptor	Homo sapiens (human)
myotube differentiation	Vasopressin V1a receptor	Homo sapiens (human)
calcium-mediated signaling	Vasopressin V1a receptor	Homo sapiens (human)
telencephalon development	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of cell growth	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of prostaglandin biosynthetic process	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of cellular pH reduction	Vasopressin V1a receptor	Homo sapiens (human)
social behavior	Vasopressin V1a receptor	Homo sapiens (human)
cellular response to water deprivation	Vasopressin V1a receptor	Homo sapiens (human)
maternal behavior	Vasopressin V1a receptor	Homo sapiens (human)
sperm ejaculation	Vasopressin V1a receptor	Homo sapiens (human)
response to corticosterone	Vasopressin V1a receptor	Homo sapiens (human)
negative regulation of transmission of nerve impulse	Vasopressin V1a receptor	Homo sapiens (human)
transport across blood-brain barrier	Vasopressin V1a receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Vasopressin V1a receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Vasopressin V1a receptor	Homo sapiens (human)
cellular response to hormone stimulus	Vasopressin V1a receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure by vasopressin	Vasopressin V1a receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Vasopressin V1b receptor	Homo sapiens (human)
activation of phospholipase C activity	Vasopressin V1b receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Vasopressin V1b receptor	Homo sapiens (human)
positive regulation of phospholipase A2 activity	Vasopressin V1b receptor	Homo sapiens (human)
regulation of cell population proliferation	Vasopressin V1b receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Vasopressin V1b receptor	Homo sapiens (human)
symbiont entry into host cell	Vasopressin V1b receptor	Homo sapiens (human)
positive regulation of inositol phosphate biosynthetic process	Vasopressin V1b receptor	Homo sapiens (human)
positive regulation of arachidonic acid secretion	Vasopressin V1b receptor	Homo sapiens (human)
transport across blood-brain barrier	Vasopressin V1b receptor	Homo sapiens (human)
cellular response to hormone stimulus	Vasopressin V1b receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure by vasopressin	Vasopressin V1b receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Vasopressin V1b receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
vasopressin receptor activity	Vasopressin V2 receptor	Homo sapiens (human)
protein binding	Vasopressin V2 receptor	Homo sapiens (human)
peptide binding	Vasopressin V2 receptor	Homo sapiens (human)
peptide hormone binding	Oxytocin receptor	Homo sapiens (human)
peptide binding	Oxytocin receptor	Homo sapiens (human)
vasopressin receptor activity	Oxytocin receptor	Homo sapiens (human)
oxytocin receptor activity	Oxytocin receptor	Homo sapiens (human)
vasopressin receptor activity	Vasopressin V1a receptor	Homo sapiens (human)
protein kinase C binding	Vasopressin V1a receptor	Homo sapiens (human)
protein binding	Vasopressin V1a receptor	Homo sapiens (human)
peptide hormone binding	Vasopressin V1a receptor	Homo sapiens (human)
V1A vasopressin receptor binding	Vasopressin V1a receptor	Homo sapiens (human)
peptide binding	Vasopressin V1a receptor	Homo sapiens (human)
vasopressin receptor activity	Vasopressin V1b receptor	Homo sapiens (human)
protein kinase C binding	Vasopressin V1b receptor	Homo sapiens (human)
peptide binding	Vasopressin V1b receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
endosome	Vasopressin V2 receptor	Homo sapiens (human)
endoplasmic reticulum	Vasopressin V2 receptor	Homo sapiens (human)
Golgi apparatus	Vasopressin V2 receptor	Homo sapiens (human)
plasma membrane	Vasopressin V2 receptor	Homo sapiens (human)
membrane	Vasopressin V2 receptor	Homo sapiens (human)
endocytic vesicle	Vasopressin V2 receptor	Homo sapiens (human)
clathrin-coated endocytic vesicle membrane	Vasopressin V2 receptor	Homo sapiens (human)
perinuclear region of cytoplasm	Vasopressin V2 receptor	Homo sapiens (human)
plasma membrane	Vasopressin V2 receptor	Homo sapiens (human)
plasma membrane	Oxytocin receptor	Homo sapiens (human)
microvillus	Oxytocin receptor	Homo sapiens (human)
adherens junction	Oxytocin receptor	Homo sapiens (human)
apical plasma membrane	Oxytocin receptor	Homo sapiens (human)
plasma membrane	Oxytocin receptor	Homo sapiens (human)
endosome	Vasopressin V1a receptor	Homo sapiens (human)
plasma membrane	Vasopressin V1a receptor	Homo sapiens (human)
endocytic vesicle	Vasopressin V1a receptor	Homo sapiens (human)
plasma membrane	Vasopressin V1a receptor	Homo sapiens (human)
endosome	Vasopressin V1b receptor	Homo sapiens (human)
Golgi apparatus	Vasopressin V1b receptor	Homo sapiens (human)
plasma membrane	Vasopressin V1b receptor	Homo sapiens (human)
plasma membrane	Vasopressin V1b receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay ID	Title	Year	Journal	Article
AID1386901	Binding affinity to OTR receptor (unknown origin)	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386918	Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced myo-inositol 1-phosphate accumulation at 1 uM by IP-One assay relative to AVP	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID260557	Antidiuretic effect measured as decrease in urine volume over control in water-loaded Sprague-Dawley rat at 10 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
AID412970	Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.
AID1386881	Binding affinity to V1A receptor (unknown origin)	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID458564	Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID458556	Activity at human oxytocin receptor expressed in CHO cells assessed as inhibition of agonist-induced inositol phosphate accumulation	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID458579	Activity at human vasopressin V2 receptor expressed in CHO cells assessed as inhibition of agonist-induced cAMP accumulation at 1 uM	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID458562	Activity at human vasopressin V1a receptor expressed in CHO cells assessed as inositol phosphate accumulation at 1 uM	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID1386914	Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP accumulation at 1 uM by cAMP dynamic 2 assay relative to AVP	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID458559	Activity at human oxytocin receptor expressed in CHO cells by NFAT-luciferase gene reporter assay	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID458566	Activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation at 1 uM	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID1386919	Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of AVP-induced cAMP accumulation at 1 uM by cAMP dynamic 2 assay relative to AVP	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386902	Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386910	Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID301768	Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21	Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
AID301770	Effect on urine volume in rat 10 mg/kg, po relative to control	2007	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21	Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
AID260564	Displacement of [3H]AVP from human V2 receptor transfected in LV2 cells	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
AID1386922	Agonist activity at human V1A receptor expressed in CHO cells assessed as increase in myo-inositol 1-phosphate accumulation at 1 uM by IP-One assay relative to AVP	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID260558	Antidiuretic effect measured as increase in osmolality over control in water-loaded Sprague-Dawley rat at 10 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
AID1386909	Displacement of [3H]-AVP from human V1A receptor expressed in CHO cell membranes by radioligand binding assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386883	Binding affinity to V2 receptor (unknown origin)	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386936	Selectivity for human OTR receptor over human V2 receptor	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386903	Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID458577	Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID458553	Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID1386917	Antagonist activity at human OTR receptor expressed in CHO cells assessed as inhibition of OT-induced myo-inositol 1-phosphate accumulation by IP-One assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386921	Agonist activity at human OTR receptor expressed in CHO cells assessed as increase in myo-inositol 1-phosphate accumulation at 1 uM by IP-One assay relative to OT	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1386882	Binding affinity to V1B receptor (unknown origin)	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID301764	Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells	2007	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21	Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
AID458565	Activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID458555	Activity at human oxytocin receptor expressed in CHO cells assessed as inositol phosphate accumulation at 1 uM	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID260560	Displacement of [3H]AVP from human V1a receptor expressed in CHO cells	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
AID301767	Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21	Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.
AID1386911	Displacement of [3H]-AVP from human OXR receptor expressed in CHO cell membranes by radioligand binding assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID458560	Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID1386904	Antagonist activity at OXR receptor in rat uterus	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID458576	Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID244068	Agonist activity against Vasopressin V2 receptor relative to Oxytocin receptor at 3 uM	2004	Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17	Non-peptide oxytocin agonists.
AID1386935	Selectivity for human V1a receptor over human V2 receptor	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID458578	Activity at human vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced inositol phosphate accumulation at 1 uM	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
AID260559	Binding to human V2 receptor expressed in LV2 cells by cAMP production	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
AID1386912	Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP accumulation by cAMP dynamic 2 assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
AID1346453	Human V2 receptor (Vasopressin and oxytocin receptors)	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (66.67)	29.6817
2010's	2 (33.33)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.03	1	pyrrole; secondary amine
conivaptan conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH).	2.17	1	benzazepine	aquaretic; vasopressin receptor antagonist
lixivaptan [no description available]	7.03	1
oxytocin Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.	2.17	1	heterodetic cyclic peptide; peptide hormone	oxytocic; vasodilator agent
arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6.	2.03	1	vasopressin	cardiovascular drug; hematologic agent; mitogen
opc 51803 OPC 51803: a nonpeptide vasopressin V(2)-agonist; structure in first source	2.47	2
atosiban [no description available]	2.03	1	oligopeptide
l 371257 L 371257: structure given in first source	2.05	1
carbetocin carbetocin : Oxytocin in which the hydrogen on the phenolic hydroxy group is substituted by methyl, the amino group on the cysteine residue is substituted by hydrogen, and the sulfur of the cysteine residue is replaced by a methylene group. A synthetic carba-analogue of oxytocin, it is used to control bleeding after giving birth. Like oxytocin, it causes contraction of the uterus.	2.17	1	heterodetic cyclic peptide	oxytocic
way 267464 [no description available]	2.17	1

Condition	Relationship Strength	Studies
Autism [description not available]	2.17	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.17	1
Autistic Disorder A disorder beginning in childhood. It is marked by the presence of markedly abnormal or impaired development in social interaction and communication and a markedly restricted repertoire of activity and interest. Manifestations of the disorder vary greatly depending on the developmental level and chronological age of the individual. (DSM-V)	2.17	1

way-151932

Description

Cross-References

Synonyms (26)

Protein Targets (6)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (69)

Molecular Functions (7)

Ceullar Components (11)

Bioassays (44)

Research

Studies (6)

Market Indicators

Research Demand Index: 12.33

Study Types

way-151932

Description

Cross-References

Synonyms (26)

Protein Targets (6)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (69)

Molecular Functions (7)

Ceullar Components (11)

Bioassays (44)

Research

Studies (6)

Market Indicators

Research Demand Index: 12.33

Study Types

Related Drugs (10)

Related Conditions (3)