Compounds > AZD1979
Page last updated: 2024-11-13

AZD1979

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Description

AZD1979: an antagonist of melanin concentrating hormone receptor 1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

AZD1979 : A carboxamide resulting from the formal condensation of the carboxy group of 5-(p-methoxyphenyl)-1,3,4-oxadiazole-2-carboxylic acid with the amino group of 3-phenoxyazetidine and in which the phenoxy group has been substituted at the para- position by a 2-oxa-6-azaspiro[3.3]heptan-6-ylmethyl group. It is a melanin concentrating hormone receptor 1 (MCHr1) antagonist. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID49801838
CHEMBL ID3787394
CHEBI ID139154
SCHEMBL ID113480

Synonyms (25)

Synonym
azd 1979
azd1979
1254035-84-1
azd-1979
CHEBI:139154
[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]{3-[4-(2-oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy]azetidin-1-yl}methanone
SCHEMBL113480
unii-h9hgk5c4um
CHEMBL3787394 ,
(3-(4-(2-oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone
bdbm50159343
methanone, (5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)(3-(4-(2-oxa-6-azaspiro(3.3)hept-6-ylmethyl)phenoxy)-1-azetidinyl)-
azd 1979 [who-dd]
H9HGK5C4UM ,
AKOS030629090
CS-7456
HY-U00257
(3-(4-((2-oxa-6-azaspiro[3.3]heptan-6-yl)methyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone
EX-A7076
SB19727
[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]-[3-[4-(2-oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy]azetidin-1-yl]methanone
MS-28503
mfcd30471075
[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl][3-[4-(2-oxa-6-azaspiro[3.3]hept-6-ylmethyl)phenoxy]-1-azetidinyl]methanone
DTXSID001106011

Research Excerpts

Overview

AZD1979 is a novel potent MCH1 receptor antagonist that affects both food intake and energy expenditure.

ExcerptReferenceRelevance
"AZD1979 is a novel potent MCH1 receptor antagonist that affects both food intake and energy expenditure. "( Effects of a novel potent melanin-concentrating hormone receptor 1 antagonist, AZD1979, on body weight homeostasis in mice and dogs.
Andersson, L; Antonsson, M; Benthem, L; Bjursell, M; Börjesson, J; Carlsson, B; Gennemark, P; Iverson, S; Johansson, A; Kakol-Palm, D; Kärrberg, L; Lindén, D; Månsson, M; Ploj, K; Turnbull, A, 2016)		2.1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
melanin-concentrating hormone receptor antagonistAn antagonist that attaches to and blocks melanin-concentrating hormone receptors.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (7)

ClassDescription
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
oxaspiro compoundA spiro compound in which at least one of the cyclic components is an oxygen heterocyle.
oxadiazole
N-acylazetidine
oxetanesAny oxacycle that is oxetane or its substituted derivatives.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
carboxamideAn amide of a carboxylic acid, having the structure RC(=O)NR2. The term is used as a suffix in systematic name formation to denote the -C(=O)NH2 group including its carbon atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)22.00000.00091.901410.0000AID1289471
Melanin-concentrating hormone receptor 1Mus musculus (house mouse)IC50 (µMol)0.01100.01100.01100.0110AID1289477
Melanin-concentrating hormone receptor 1Homo sapiens (human)IC50 (µMol)0.02700.00050.23633.5000AID1289469
Histamine H3 receptorHomo sapiens (human)IC50 (µMol)0.40000.00050.46685.9000AID1289497
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (35)

Processvia Protein(s)Taxonomy
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
neuropeptide signaling pathwayMelanin-concentrating hormone receptor 2Homo sapiens (human)
generation of precursor metabolites and energyMelanin-concentrating hormone receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationMelanin-concentrating hormone receptor 1Homo sapiens (human)
feeding behaviorMelanin-concentrating hormone receptor 1Homo sapiens (human)
positive regulation of calcium ion transportMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuropeptide signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
G protein-coupled peptide receptor activityMelanin-concentrating hormone receptor 2Homo sapiens (human)
signaling receptor bindingMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuropeptide receptor activityMelanin-concentrating hormone receptor 1Homo sapiens (human)
melanin-concentrating hormone receptor activityMelanin-concentrating hormone receptor 1Homo sapiens (human)
hormone bindingMelanin-concentrating hormone receptor 1Homo sapiens (human)
G protein-coupled receptor activityMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuropeptide bindingMelanin-concentrating hormone receptor 1Homo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneMelanin-concentrating hormone receptor 2Homo sapiens (human)
plasma membraneMelanin-concentrating hormone receptor 2Homo sapiens (human)
plasma membraneMelanin-concentrating hormone receptor 1Homo sapiens (human)
ciliumMelanin-concentrating hormone receptor 1Homo sapiens (human)
ciliary membraneMelanin-concentrating hormone receptor 1Homo sapiens (human)
non-motile ciliumMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuron projectionMelanin-concentrating hormone receptor 1Homo sapiens (human)
plasma membraneMelanin-concentrating hormone receptor 1Homo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay IDTitleYearJournalArticle
AID1289518Cardiovascular toxicity in dog assessed as effect on heart rate up to free plasma level of 3 uM2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289507Clearance in diet-induced obese C57BL/6J mouse at 5 to 50 umol/kg, bid administered via oral gavage after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289487Fraction unbound in dog plasma2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289523Dissociation constant, pKa of the compound2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289520Cardiovascular toxicity in dog assessed as effect on QT up to free plasma level of 3 uM2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516561Substrate activity at mEH in human liver microsomes assessed as diol release at 10 uM measured after 60 mins in presence of NADPH by UPLC-Q-TOF/MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1516563Substrate activity at mEH in human liver microsomes assessed as amino alcohol release at 10 uM measured after 60 mins in presence of NADPH by UPLC-Q-TOF/MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289509Relative bioavailability in diet-induced obese C57BL/6J mouse at 5 umol/kg, bid administered via oral gavage after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289511Absorption rate constant in diet-induced obese C57BL/6J mouse at 5 to 50 umol/kg, bid administered via oral gavage after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289515Cardiovascular toxicity in guniea pig assessed as effect on heart rate up to free plasma level of 3 uM2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289519Cardiovascular toxicity in dog assessed as effect on blood pressure up to free plasma level of 3 uM2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289505Toxicity in DIO C57BL/6J mouse deficient of MCHr1 assessed as effect on food intake2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289506Toxicity in DIO C57BL/6J mouse deficient of MCHr1 assessed as effect on body weight2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289474Lipophilicity, log D of the compound at pH 7.4 by HPLC analysis2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516555Drug metabolism in human liver microsomes assessed as mEH-mediated oxidoreductive ring-opening of azetidine by measuring [3-[4-[[[3-(hydroxymethyl)oxetan-3-yl]methylamino]methyl]phenoxy]azetidin-1-yl]-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]methanone fo2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289492Volume of distribution in steady state in dog2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289504Decrease in body weight in diet-induced obese C57BL/6J mouse at 5 umol/kg, bid administered via oral gavage after 20 days relative to vehicle control2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289510Relative bioavailability in diet-induced obese C57BL/6J mouse at 20 to 50 umol/kg, bid administered via oral gavage after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289495Oral bioavailability in rat2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289508Volume of distribution in diet-induced obese C57BL/6J mouse at 5 to 50 umol/kg, bid administered via oral gavage after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289512EX vivo receptor occupancy at MCHR1 in diet-induced obese C57BL/6J mouse brain assessed as dissociation constant administered via oral gavage, bid after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289486Fraction unbound in rat plasma2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516559Dissociation constant, pKa of compound at pH 2.3 to 10.8 by pressure assisted capillary electrophoresis-MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289524Toxicity in rat up to 100 mg/kg after 1 month by GLP study2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289494Half life in dog2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289517Cardiovascular toxicity in guniea pig assessed as effect on QT up to free plasma level of 3 uM2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289491Volume of distribution in steady state in rat2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289496Oral bioavailability in dog2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289484Intrinsic clearance in dog hepatocytes assessed per 10'6 cells2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289475Intrinsic clearance in human liver microsomes2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289490Clearance in dog2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516557Aqueous solubility of the compound in pH 7.4 HBSS buffer HPLC-MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289525Toxicity in dog up to 100 mg/kg after 1 month by GLP study2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516558Octanol-water distribution coefficient, log D of the compound at pH 7.4 by RP-HPLC analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289529Drug metabolism in human liver microsomes by KCN trapping assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289467Decrease in body weight in diet-induced obese C57BL/6J mouse at 20 to 50 umol/kg, bid administered via oral gavage after 20 days relative to vehicle control2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516560Intrinsic clearance in human hepatocytes assessed per million cells at 50 uM in presence of NADPH by HPLC-MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1630394Dissociation constant, pKa of the compound2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Evolution of physicochemical properties of melanin concentrating hormone receptor 1 (MCHr1) antagonists.
AID1289527Time-dependent inhibition of CYP450 (unknown origin)2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289468Efflux ratio of permeability in human Caco2 cells2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289493Half life in rat2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289485Intrinsic clearance in human hepatocytes assessed per 10'6 cells2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289477Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516556Drug metabolism in human liver microsomes assessed as mEH-mediated hydrolytic ring-opening of oxetane by measuring [3-[4-[[3,3-bis(hydroxymethyl)azetidin-1-yl]methyl]phenoxy]azetidin-1-yl]-[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]methanone formation by U2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289489Clearance in rat2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289528Drug metabolism in human liver microsomes assessed as reactive metabolite formation from GSH2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289471Inhibition of human ERG by IonWork assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289488Fraction unbound in human plasma2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1516562Substrate activity at mEH in human liver microsomes assessed as diol release at 10 uM measured after 60 mins in absence of NADPH by UPLC-Q-TOF/MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Hip To Be Square: Oxetanes as Design Elements To Alter Metabolic Pathways.
AID1289469Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289483Intrinsic clearance in rat hepatocytes assessed per 10'6 cells2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289516Cardiovascular toxicity in guniea pig assessed as effect on blood pressure up to free plasma level of 3 uM2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289526Reversible inhibition of CYP450 (unknown origin)2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289514Antagonist activity at human MCHR2 expressed in CHO cells after 60 to 75 mins by FLIPR assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289479Ex vivo receptor occupancy at MCHR1 in po dosed C57BL/6J mouse brain assessed as mouse free plasma level based IC50 measured up to 24 hrs post dose by tritium imaging plate analysis in presence of [3H]-SNAP-79412016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289497Inhibition of histamine H3 receptor (unknown origin)2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289482Permeability from apical to basolateral side in human Caco2 cells2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
AID1289513EX vivo receptor occupancy at MCHR1 in diet-induced obese C57BL/6J mouse brain assessed as dissociation rate constant administered via oral gavage, bid after 20 days2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.61 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.1310amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
progabide
progabide: GABA agonist; structure		2.1310diarylmethane
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		3.2450
ConditionIndicatedRelationship StrengthStudiesTrials
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		07.8330
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		07.1510