Page last updated: 2024-11-13

azd7687

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Description

AZD7687: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID42636350
CHEMBL ID2178953
CHEMBL ID2178944
CHEMBL ID4297354
SCHEMBL ID5532381
SCHEMBL ID2252415
SCHEMBL ID2255196
SCHEMBL ID2252417
MeSH IDM0581615

Synonyms (36)

Synonym
chembl2178953 ,
bdbm50399684
chembl2178944 ,
bdbm50399710
HY-15497
azd7687
CS-1026
azd 7687
gtpl7827
azd-7687
1166827-44-6
SCHEMBL5532381
SCHEMBL2252415
SCHEMBL2255196
SCHEMBL2252417
DTXSID60655297
{4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid
AKOS030526281
trans-4-(4-(6-(aminocarbonyl)-3,5-dimethyl-2-pyrazinyl)phenyl)cyclohexaneacetic acid
6QTJ9P2NYT ,
azd 7687 [who-dd]
NCGC00378858-01
unii-6qtj9p2nyt
DB14949
Q27074787
{trans-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid
YXFNPRHZMOGREC-SHTZXODSSA-N
CHEMBL4297354
F84876
MS-25885
2-[4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
2-((1s,4s)-4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid
trans-{4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid
2-(4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid
A926420
GLXC-26148

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
" Meal fat content or data from single vs repeated dosing did not affect model parameter estimates."( Evolving data analysis of an Oral Lipid Tolerance Test toward the standard for the Oral Glucose Tolerance Test: Cross species modeling effects of AZD7687 on plasma triacylglycerol.
Birtles, S; Morentin Gutierrez, P; Nilsson, C; Yates, J, 2019
)
0.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50 (µMol)3.70000.00020.59827.0000AID709001
Diacylglycerol O-acyltransferase 1Homo sapiens (human)IC50 (µMol)100.08830.00050.04300.4300AID1546904; AID709030; AID709031; AID709046
Sterol O-acyltransferase 2Homo sapiens (human)IC50 (µMol)10.00000.11003.20369.2000AID709029
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)30.00000.00011.774010.0000AID709020
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)80.50000.00001.23267.7930AID709000
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)30.00000.00011.753610.0000AID709016
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)30.00000.00002.015110.0000AID709017
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)30.00000.00002.800510.0000AID709019
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)30.00000.00002.398310.0000AID709018
Sterol O-acyltransferase 1Homo sapiens (human)IC50 (µMol)34.00000.02501.79758.0000AID709042
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)32.00000.00091.901410.0000AID709021
Diacylglycerol O-acyltransferase 2Homo sapiens (human)IC50 (µMol)150.04000.00130.03180.0800AID1546895; AID709030
Diacylglycerol O-acyltransferase 1Rattus norvegicus (Norway rat)IC50 (µMol)31.00000.00050.03230.0640AID709017; AID709021
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)IC50 (µMol)5.50000.00001.49049.2000AID708999
Diacylglycerol O-acyltransferase 1Mus musculus (house mouse)IC50 (µMol)30.00000.00110.01400.0240AID709017
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (105)

Processvia Protein(s)Taxonomy
fatty acid catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
arachidonic acid metabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
positive regulation of vasoconstrictionFatty-acid amide hydrolase 1Homo sapiens (human)
monoacylglycerol catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
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)
cholesterol metabolic processSterol O-acyltransferase 2Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 2Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 2Homo sapiens (human)
intestinal cholesterol absorptionSterol O-acyltransferase 2Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 2Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 2Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 2Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 2Homo 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)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo 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)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 1Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 1Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 1Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 1Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 1Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 1Homo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic processSterol O-acyltransferase 1Homo 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)
glycerol metabolic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
monoacylglycerol biosynthetic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
diacylglycerol biosynthetic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
triglyceride biosynthetic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
lipid storageDiacylglycerol O-acyltransferase 2Homo sapiens (human)
low-density lipoprotein particle clearanceDiacylglycerol O-acyltransferase 2Homo sapiens (human)
long-chain fatty-acyl-CoA metabolic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
intracellular triglyceride homeostasisDiacylglycerol O-acyltransferase 2Homo sapiens (human)
retinol metabolic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
cholesterol homeostasisDiacylglycerol O-acyltransferase 2Homo sapiens (human)
diacylglycerol metabolic processDiacylglycerol O-acyltransferase 2Homo sapiens (human)
fatty acid homeostasisDiacylglycerol O-acyltransferase 2Homo sapiens (human)
fat pad developmentDiacylglycerol O-acyltransferase 2Homo sapiens (human)
cellular response to oleic acidDiacylglycerol O-acyltransferase 2Homo sapiens (human)
regulation of plasma lipoprotein particle levelsDiacylglycerol O-acyltransferase 2Homo sapiens (human)
cAMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
negative regulation of cGMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (67)

Processvia Protein(s)Taxonomy
protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
phospholipid bindingFatty-acid amide hydrolase 1Homo sapiens (human)
fatty acid amide hydrolase activityFatty-acid amide hydrolase 1Homo sapiens (human)
identical protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
acylglycerol lipase activityFatty-acid amide hydrolase 1Homo sapiens (human)
amidase activityFatty-acid amide hydrolase 1Homo sapiens (human)
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)
fatty-acyl-CoA bindingSterol O-acyltransferase 2Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
protein bindingSterol O-acyltransferase 2Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 2Homo sapiens (human)
acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 2Homo 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)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo 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)
fatty-acyl-CoA bindingSterol O-acyltransferase 1Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
protein bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 1Homo 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)
2-acylglycerol O-acyltransferase activityDiacylglycerol O-acyltransferase 2Homo sapiens (human)
diacylglycerol O-acyltransferase activityDiacylglycerol O-acyltransferase 2Homo sapiens (human)
protein bindingDiacylglycerol O-acyltransferase 2Homo sapiens (human)
protein homodimerization activityDiacylglycerol O-acyltransferase 2Homo sapiens (human)
retinol O-fatty-acyltransferase activityDiacylglycerol O-acyltransferase 2Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
metal ion bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneFatty-acid amide hydrolase 1Homo sapiens (human)
cytoskeletonFatty-acid amide hydrolase 1Homo sapiens (human)
organelle membraneFatty-acid amide hydrolase 1Homo sapiens (human)
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 reticulumSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 2Homo sapiens (human)
brush borderSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 2Homo 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)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo 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)
endoplasmic reticulumSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
membraneSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo 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)
mitochondrionDiacylglycerol O-acyltransferase 2Homo sapiens (human)
lipid dropletDiacylglycerol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulumDiacylglycerol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneDiacylglycerol O-acyltransferase 2Homo sapiens (human)
lipid dropletDiacylglycerol O-acyltransferase 2Homo sapiens (human)
cytosolDiacylglycerol O-acyltransferase 2Homo sapiens (human)
membraneDiacylglycerol O-acyltransferase 2Homo sapiens (human)
intracellular membrane-bounded organelleDiacylglycerol O-acyltransferase 2Homo sapiens (human)
perinuclear region of cytoplasmDiacylglycerol O-acyltransferase 2Homo sapiens (human)
perinuclear endoplasmic reticulum membraneDiacylglycerol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneDiacylglycerol O-acyltransferase 2Homo sapiens (human)
cytosolcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID709011Intrinsic clearance in dog hepatocytes assessed as parent compound disappearance at 1 uM per 10'6 cells2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709004Half life in Beagle dog at 27.2 uM/kg, po2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1062223Reduction of triglyceride AUC in human at 60 mg2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.
AID709028Inhibition of DGAT1 in rat liver microsomes2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709027Inhibition of DGAT1 in rat adipose tissue assessed as reduction in triacylglycerol synthesis2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709044Octanol/water partition coefficient, log D of the compound at pH 7.42012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709000Inhibition of muscarinic M2 receptor2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709021Inhibition of human ERG2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1546895Inhibition of recombinant FLAG-tagged human DGAT2 expressed in SF9 cells after 1 hr by TopCount assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
AID708993Terminal half life in human at 1 to 20 mg2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709017Inhibition of CYP2D62012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709014Intrinsic clearance in human hepatocytes assessed as parent compound disappearance at 1 uM per 10'6 cells2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID708996Inhibition of plasma triacylglycerol excursion in 14 hrs fasted Han-Wistar rat at administered orally 2 hrs before bolus corn oil administration measured 1.5 hrs post corn oil challenge by oral lipid tolerance test relative to control2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709013Photostability stability by Hanau sun test2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709016Inhibition of CYP3A42012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1062226Tmax in human2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.
AID709043Volume of distribution in C57BL/6 mouse at 8.16 uM/kg, po or 5.4 uM/kg, iv2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709025Fraction unbound in rat plasma2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1062225Terminal half life in human2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.
AID709015Chemical stability in pH 1 to 10 buffer at 25 degC2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709033Inhibition of DGAT1 in human liver microsomes2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709003Oral bioavailability in Beagle dog at 27.2 uM/kg2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID708994Tmax in human at 1 to 20 mg2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709024Inhibition of DGAT1 in dog liver microsomes2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709006Clearance in Beagle dog at 27.2 uM/kg, po or 1.4 uM/kg, iv2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1062224Reduction of triglyceride AUC in human receiving 60% fat meal at >5 mg2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.
AID709005Volume of distribution in Beagle dog at 27.2 uM/kg, po or 1.4 uM/kg, iv2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709001Inhibition of FAAH2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709032Inhibition of DGAT1 in human adipose tissue assessed as reduction in triacylglycerol synthesis2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709008Clearance in Han-Wistar rat at 5.4 uM/kg, po or 2.7 uM/kg, iv2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709012Intrinsic clearance in mouse hepatocytes assessed as parent compound disappearance at 1 uM per 10'6 cells2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709009Oral bioavailability in C57BL/6 mouse at 8.16 uM/kg2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709038Apparent permeability from apical to basolateral side in MDCK cells at pH 7.42012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709041Solubility in 0.1 M phosphate buffer at pH 7.4 at 25 degC incubated for 24 hrs2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709010Half life in C57BL/6 mouse at 8.16 uM/kg, po2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID708999Inhibition of PDE10A1 receptor2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1546904Inhibition of recombinant FLAG-tagged human DGAT1 expressed in SF9 cells after 1 hr by TopCount assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
AID709018Inhibition of CYP2C192012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1062220Reduction of triglyceride AUC in human relative to baseline2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.
AID709046Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709002Inhibition of ACAT at 10 uM2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709026Inhibition of DGAT1 in mouse liver microsomes2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709023Fraction unbound in mouse plasma2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709007Volume of distribution in Han-Wistar rat at 5.4 uM/kg, po or 2.7 uM/kg, iv2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709039Intrinsic clearance in rat hepatocytes assessed as parent compound disappearance at 1 uM per 10'6 cells2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709022Fraction unbound in dog plasma2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709031Inhibition of DGAT1 in human HuTu80 cells2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709030Inhibition of human DGAT2 by liquid scintillography2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID708995Inhibition of adipose triacylglycerol synthesis in 14 hrs fasted Han-Wistar rat assessed as decrease in ratio of [3H]palmitic acid incorporation in to TAG and DAG at 8 mg/kg administered orally and measured 1.5 hrs post dose relative to control2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709020Inhibition of CYP1A22012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709035Half life in Han-Wistar rat at 2.54 to 5.4 uM/kg, po2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709042Inhibition of human ACAT1 by liquid scintillography2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709029Inhibition of human ACAT2 by liquid scintillography2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709040Fraction unbound in human plasma at 37 degC by LC-UV/MS method based equilibrium dialysis method2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1062222Reduction of triglyceride AUC in human2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors.
AID709019Inhibition of CYP2C92012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709047Clearance in C57BL/6 mouse at 8.16 uM/kg, po or 5.4 uM/kg, iv2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID708992Reduction in serum triglyceride level in human on standardized mixed meal diet at 5 mg UID2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID709034Oral bioavailability in rat2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
AID1346154Human diacylglycerol O-acyltransferase 1 (2.3.1.- Acyltransferases)2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
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.
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.
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.
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.
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.
AID709045Lipophilicity, log D of the compound at pH 7.4 by chromatographic method2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (72.73)24.3611
2020's3 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.05

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 Index17.05 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (18.18%)5.53%
Reviews2 (18.18%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (63.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]