Page last updated: 2024-11-13

azd3988

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

Description

AZD3988: for treatment of obesity and diabetes; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23648867
CHEMBL ID2036730
SCHEMBL ID3543235
SCHEMBL ID3543232
SCHEMBL ID24454495
MeSH IDM0577273

Synonyms (19)

Synonym
bdbm50385398
azd-3988
CHEMBL2036730 ,
trans-4-[4-[[[5-[(3,4-difluorophenyl)amino]-1,3,4-oxadiazol-2-yl]carbonyl]amino]phenyl]cyclohexaneacetic acid
892489-52-0
SCHEMBL3543235
SCHEMBL3543232
AKOS025142026
trans-4-[-[[[5-[(3,4-difluorophenyl)amino]-1,3,4-oxadiazol-2-yl]carbonyl]amino]phenyl]cyclohexaneacetic acid
azd 3988
trans-4-[4-[[[5-[(3,4-difluorophenyl)amino]-1,3,4-oxadiazol-2-yl]carbonyl]amino]phenyl]-cyclohexaneacetic acid
NCGC00387203-01
FT-0755333
HY-50861
azd3988
CS-0004334
MS-28319
2-[4-[4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl]cyclohexyl]acetic acid
SCHEMBL24454495

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
" Compound 23n conferred weight loss and a reduction in liver triglycerides when dosed chronically in mice with diet-induced obesity and depleted serum triglycerides following a lipid challenge."( Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
Aslanian, R; Cook, J; Hwa, J; Lachowicz, J; Lin, A; Lin, M; Smith, M; Ting, P; van Heek, M; Walker, S; Zhou, G; Zorn, N, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Diacylglycerol O-acyltransferase 1Homo sapiens (human)IC50 (µMol)0.01830.00050.04300.4300AID1129956; AID1154993; AID665873; AID665880
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)30.00000.00011.774010.0000AID665886
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)30.00000.00011.753610.0000AID665890
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)30.00000.00002.015110.0000AID665889
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)30.00000.00002.800510.0000AID665887
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)30.00000.00002.398310.0000AID665888
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)30.00000.00091.901410.0000AID665885
Diacylglycerol O-acyltransferase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.00050.00050.03230.0640AID665878
Diacylglycerol O-acyltransferase 1Mus musculus (house mouse)IC50 (µMol)0.00110.00110.01400.0240AID665879
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

Processvia Protein(s)Taxonomy
triglyceride biosynthetic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
monoacylglycerol biosynthetic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
triglyceride metabolic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
triglyceride biosynthetic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
lipid storageDiacylglycerol O-acyltransferase 1Homo sapiens (human)
very-low-density lipoprotein particle assemblyDiacylglycerol O-acyltransferase 1Homo sapiens (human)
long-chain fatty-acyl-CoA metabolic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
retinol metabolic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
diacylglycerol metabolic processDiacylglycerol O-acyltransferase 1Homo sapiens (human)
fatty acid homeostasisDiacylglycerol O-acyltransferase 1Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo 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)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
2-acylglycerol O-acyltransferase activityDiacylglycerol O-acyltransferase 1Homo sapiens (human)
diacylglycerol O-acyltransferase activityDiacylglycerol O-acyltransferase 1Homo sapiens (human)
protein bindingDiacylglycerol O-acyltransferase 1Homo sapiens (human)
acyltransferase activityDiacylglycerol O-acyltransferase 1Homo sapiens (human)
identical protein bindingDiacylglycerol O-acyltransferase 1Homo sapiens (human)
retinol O-fatty-acyltransferase activityDiacylglycerol O-acyltransferase 1Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo 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 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo 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)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo 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 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo 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 2C19Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneDiacylglycerol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneDiacylglycerol O-acyltransferase 1Homo sapiens (human)
plasma membraneDiacylglycerol O-acyltransferase 1Homo sapiens (human)
membraneDiacylglycerol O-acyltransferase 1Homo sapiens (human)
specific granule membraneDiacylglycerol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo 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)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (54)

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.
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.
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.
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.
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.
AID665899Half life in rat at 2 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665889Inhibition of CYP2D62012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665921Antiobesity activity in po dosed fasted rat assessed as reduction in TAG to DAG ratio in adipose tissue2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665909Antiobesity activity in fasted rat assessed as reduction in plasma triacylglycerol excursion at 0.03 mg/kg, po administered 2 hrs prior to bolus dose of corn oil measured after 1.5 hrs by OLTT2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665895Cmax in mouse at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665882Fraction unbound in rat plasma2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665883Apparent permeability across apical to basolateral side in MDCK cells at 10 uM2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665917Antiobesity activity in DIO mouse assessed as reduction in body weight at 20 mg/kg, po bid for 3 days2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665912Antiobesity activity in po dosed fasted rat assessed as reduction in plasma triacylglycerol excursion administered 2 hrs prior to bolus dose of corn oil measured after 1.5 hrs by OLTT2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665886Inhibition of CYP1A22012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665879Inhibition of mouse DGAT12012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665894Half life in mouse at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665893Half life in mouse at 0.5 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665902Oral bioavailability in rat at 5 mg/kg2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665898Volume of distribution at steady state in rat at 2 mg/kg, iv and 5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665873Inhibition of human recombinant DGAT1 expressed in baculovirus infected insect sf9 cells using [14C] oleoyl coenzyme A after 30 mins by scintillation counting2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665903Plasma clearance in dog at 1 mg/kg, iv and 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665880Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665885Inhibition of human Erg2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665914Antiobesity activity in fasted rat assessed as reduction in TAG to DAG ratio in adipose tissue at 0.3 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665911Antiobesity activity in fasted rat assessed as reduction in plasma triacylglycerol excursion at 0.2 mg/kg, po administered 2 hrs prior to bolus dose of corn oil measured after 1.5 hrs by OLTT2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665905Half life in rat at dog at 1 mg/kg, iv2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665892Volume of distribution at steady state in mouse at 0.5 mg/kg, iv and 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665907Cmax in dog at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665906Half life in dog at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665915Antiobesity activity in fasted rat assessed as reduction in TAG to DAG ratio in adipose tissue at 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665904Volume of distribution at steady state in dog at 1 mg/kg, iv and 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665875Lipophilicity, log D of the compound2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665900Half life in rat at 5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665913Antiobesity activity in fasted rat assessed as reduction in TAG to DAG ratio in adipose tissue at 0.1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665896Oral bioavailability in mouse at 1 mg/kg2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665901Cmax in rat at 5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665884Apparent permeability across basolateral to apical side in MDCK cells at 10 uM2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665877Aqueous solubility of the compound at pH 7.42012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665881Fraction unbound in human plasma2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665919Antiobesity activity in DIO mouse assessed as reduction in food intake at 20 mg/kg, po bid for 3 days2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665918Antiobesity activity in lean mouse assessed as reduction in body weight at 20 mg/kg, po bid for 3 days2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665887Inhibition of CYP2C92012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665897Plasma clearance in rat at 2 mg/kg, iv and 5 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID1154993Inhibition of human DGAT1 expressed in Sf9 insect cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-CoA substrate by scintillation counting analysis2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
AID665908Oral bioavailability in dog at 1 mg/kg2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665890Inhibition of CYP3A42012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665874Inhibition of DGAT2 expressed in baculovirus infected insect sf9 cells using [14C] oleoyl coenzyme A at 10 uM after 30 mins by scintillation counting2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665878Inhibition of rat DGAT12012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665916Antiobesity activity in fasted rat assessed as reduction in TAG to DAG ratio in adipose tissue at 3 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID1129956Inhibition of human DGAT12014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.
AID665910Antiobesity activity in fasted rat assessed as reduction in plasma triacylglycerol excursion at 0.1 mg/kg, po administered 2 hrs prior to bolus dose of corn oil measured after 1.5 hrs by OLTT2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665888Inhibition of CYP2C192012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
AID665891Plasma clearance in mouse at 0.5 mg/kg, iv and 1 mg/kg, po2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
[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's5 (71.43)24.3611
2020's2 (28.57)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%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]