Page last updated: 2024-11-13

yil 781

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

YIL 781: an appetite suppressant and weight loss promoter; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23631116
CHEMBL ID243001
SCHEMBL ID2742704
MeSH IDM0515840

Synonyms (19)

Synonym
CHEMBL243001 ,
bdbm50222869
6-(4-fluorophenoxy)-3-{[(3s)-1-isopropylpiperidin-3-yl]methyl}-2-methylquinazolin-4(3h)-one
6-(4-fluorophenoxy)-2-methyl-3-[[(3s)-1-propan-2-ylpiperidin-3-yl]methyl]quinazolin-4-one
gtpl3538
yil-781
yil781
875258-85-8
yil 781
SCHEMBL2742704
NCGC00370967-01
6-(4-fluorophenoxy)-2-methyl-3-[[(3s)-1-(1-methylethyl)-3piperidinyl]methyl]-4(3h)-quinazolinone
EX-A3762
Q27089257
(s)-6-(4-fluorophenoxy)-3-((1-isopropylpiperidin-3-yl)methyl)-2-methylquinazolin-4(3h)-one
GLXC-25348
AKOS040745423
HY-13964
CS-0009014

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Starting from an agonist with poor oral bioavailability, optimization led to potent, selective, and orally bioavailable antagonists."( Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
Bierer, DE; Bloomquist, BT; Bondar, G; Brands, M; Bullock, WH; Chen, L; Chuang, CY; Claus, TH; Coish, PD; Esler, WP; Fathi, Z; Fu, W; Gardell, SJ; Khire, UR; Kristie, JA; Liu, XG; Livingston, JN; Lowe, DB; McClure, AC; Michels, M; O'connor, S; Ortiz, AA; Ramsden, PD; Rudolph, J; Schoenleber, RW; Shelekhin, TE; Sweet, LJ; Tang, W; Vakalopoulos, A; Wang, L; Wickens, PL; Yi, L, 2007
)
0.34
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Using an in vitro experimental approach, the physiological role of the airway epithelium on smooth muscle relaxation has been investigated by analyzing the dose-response curves for carbachol- or histamine-induced contractions on epithelium intact versus denuded tracheal tissue."( Relaxant effect of ghrelin on guinea pig isolated tracheal smooth muscle: role of epithelial NO and PGE
Al-Ayed, MSZ, 2018
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)13.00000.00002.015110.0000AID298509
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki1.00000.00010.954910.0000AID298507
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)1.61090.00091.901410.0000AID648796
GH-releasing peptide receptor Ovis aries (sheep)Ki0.01700.01700.01700.0170AID298501
Growth hormone secretagogue receptor type 1Homo sapiens (human)Ki0.00400.00020.03360.0906AID648794
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2AHomo sapiens (human)Activity1.00000.00030.00430.0071AID298532
5-hydroxytryptamine receptor 2BHomo sapiens (human)Activity1.00000.00260.00260.0026AID298533
Growth hormone secretagogue receptor type 1Homo sapiens (human)Kbapp0.01100.01100.01100.0110AID298503
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (156)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMotilin receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
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)
G protein-coupled receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
spermatogenesisGrowth hormone secretagogue receptor type 1Homo sapiens (human)
learning or memoryGrowth hormone secretagogue receptor type 1Homo sapiens (human)
actin polymerization or depolymerizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
adult feeding behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
hormone-mediated signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of norepinephrine secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
growth hormone secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to foodGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of appetiteGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of appetiteGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to follicle-stimulating hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to estradiolGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of interleukin-1 beta productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of interleukin-6 productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of tumor necrosis factor productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to insulin stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
ghrelin secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of multicellular organism growthGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of hindgut contractionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of fatty acid metabolic processGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of insulin secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
decidualizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of inflammatory responseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of synapse assemblyGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of transmission of nerve impulseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of growth hormone secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to growth hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to lipopolysaccharideGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to dexamethasoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of locomotion involved in locomotory behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to thyroid hormone stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of neurotransmitter receptor localization to postsynaptic specialization membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of postsynapse organizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of small intestinal transitGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to L-glutamateGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of sprouting angiogenesisGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of eating behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of small intestine smooth muscle contractionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of gastric motilityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to insulin-like growth factor stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of macrophage apoptotic processGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
G protein-coupled peptide receptor activityMotilin receptorHomo sapiens (human)
hormone bindingMotilin receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
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)
growth hormone secretagogue receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
G protein-coupled receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
growth hormone-releasing hormone receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
peptide hormone bindingGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

Processvia Protein(s)Taxonomy
cytosolMotilin receptorHomo sapiens (human)
plasma membraneMotilin receptorHomo sapiens (human)
plasma membraneMotilin receptorHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
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 membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cell surfaceGrowth hormone secretagogue receptor type 1Homo sapiens (human)
neuron projectionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
membrane raftGrowth hormone secretagogue receptor type 1Homo sapiens (human)
synaptic membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
Schaffer collateral - CA1 synapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
postsynapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
glutamatergic synapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
plasma membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID298509Inhibition of CYP2D62007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298520Cmax in Wistar rat plasma at 1 mg/kg, iv2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298516AUC in Wistar rat plasma at 3 mg/kg, po2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298503Antagonist activity at human recombinant GHSR1a expressed in HEK293F cells by [35S]GTP-gamma-S binding assay2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298527Decrease in body weight in DIO C57BL/6 mouse at 30 mg/kg, po after 9 days2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298535Binding affinity to calcium channel L type2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID648799Inhibition of muscarinic M2 receptor at 10 uM2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
AID298528Cmax in po dosed DIO C57BL/6 mouse after 5 hrs2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298529Drug level in po dosed DIO C57BL/6 mouse brain after 5 hrs relative to plasma concentration2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298517Cmax in Wistar rat plasma at 3 mg/kg, po2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298521Half life in Wistar rat plasma at 1 mg/kg, iv2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298505Cmax in Wistar rat at 3 mg/kg, po2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID648798Inhibition of muscarinic M1 receptor at 10 uM2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
AID298502Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298522Volume of distribution in Wistar rat plasma at 1 mg/kg, iv2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298530Increase in food intake in DIO C57BL/6 mouse at 30 mg/kg, after 5 hrs relative to control2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID648797Inhibition of 5-HT2B at 10 uM2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
AID648796Inhibition of human Erg by patch clamp assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
AID298531Decrease in blood glucose level in DIO Wistar rat using at 10 mg/kg after 5 hrs by IPGTT test relative to control2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298524Decrease in food intake in DIO C57BL/6 mouse at 30 mg/kg, po after 24 hrs relative to control2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298501Displacement of [125I]ghrelin from ovine recombinant GHSR1a expressed in HEK293F cells after 6 hrs by scintillation proximity assay2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298508Aqueous solubility at pH 7.22007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298534Binding affinity to motilin receptor2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298506Clearance in Wistar rat at 1 mg/kg iv2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298507Displacement of [125I]DIO from 5HT2c receptor2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID648794Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
AID298519AUC (0-t) in Wistar rat plasma at 1 mg/kg, iv2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298533Binding affinity to 5HT2b receptor2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID298518Bioavailability in Wistar rat plasma at 3 mg/kg, po2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID648795Antagonist activity at mouse GSH-R1a receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced calcium mobilization after 5 mins by FLIPR assay2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Substituted azaquinazolinones as modulators of GHSr-1a for the treatment of type II diabetes and obesity.
AID298532Binding affinity to 5HT2a receptor2007Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.
AID1346009Human ghrelin receptor (Ghrelin receptor)2007Endocrinology, Nov, Volume: 148, Issue:11
Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (11.76)29.6817
2010's12 (70.59)24.3611
2020's3 (17.65)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]