Page last updated: 2024-11-13

jnj-40411813

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Description

1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone: an mGlu2 receptor modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25195461
CHEMBL ID3337527
SCHEMBL ID1035416
MeSH IDM000602105

Synonyms (43)

Synonym
bdbm50051408
chembl3337527 ,
SCHEMBL1035416
HY-15748
CS-3357
jnj-40411813
1127498-03-6
jnj 40411813 ,
HYOGJHCDLQSAHX-UHFFFAOYSA-N ,
1'-butyl-3'-chloro-4-phenyl-3,4,5,6-tetrahydro-2h,1 'h-[1,4']bipyridinyl-2'-one
1'-butyl-3'-chloro-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-one
1'-butyl-3'-chloro-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4]bipyridinyl-2'-one
612BYT76F3 ,
1'-butyl-3'-chloro-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-(1,4')bipyridinyl-2'-one
2(1h)-pyridinone, 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-
1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2-one
jnj40411813
adx71149
adx-71149
gtpl8946
1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-2(1h)-pyridinone
1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1h)-pyridone
unii-612byt76f3
1-butyl-3-chloro-4-(4-phenylpiperidin-1-yl)pyridin-2(1h)-one
NCGC00485897-01
DB12059
FT-0752754
Q27895859
jnj-40411813; jnj 40411813; adx71149; adx 71149; adx-71149
BCP23709
EX-A2902
jnj-40411813; adx-71149
SB16990
adx 71149
A894527
F85059
MS-25297
adx-71149adx-71149
AC-35478
HZR ,
1-butyl-3-chloranyl-4-(4-phenylpiperidin-1-yl)pyridin-2-one
CVB49803
DTXSID601032323

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacological and pharmacokinetic properties of a novel mGlu2 receptor-positive allosteric modulator (PAM), 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-2(1H)-pyridinone (JNJ-40411813/ADX71149) are described here."( Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.
Ahnaou, A; Drinkenburg, W; Langlois, X; Lavreysen, H; Le Poul, E; Lütjens, R; Mackie, C; Nuñez, JM; Pype, S; Trabanco, AA, 2015
)
0.86

Bioavailability

ExcerptReferenceRelevance
"5 h) with an absolute oral bioavailability of 31%."( Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.
Ahnaou, A; Drinkenburg, W; Langlois, X; Lavreysen, H; Le Poul, E; Lütjens, R; Mackie, C; Nuñez, JM; Pype, S; Trabanco, AA, 2015
)
0.67
"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
" The present paper addresses the effects on vigilance states of the mGluR2 positive allosteric modulator (PAM) JNJ-40411813 at different circadian times in rats and after afternoon dosing in humans."( Translational neurophysiological markers for activity of the metabotropic glutamate receptor (mGluR2) modulator JNJ-40411813: Sleep EEG correlates in rodents and healthy men.
Ahnaou, A; Cid, JM; de Boer, P; Drinkenburg, WH; Huysmans, H; Kemp, JA; Lavreysen, H; Macdonald, GJ; Raeymaekers, L; Sinha, V; Van De Casteele, T; Van Nueten, L, 2016
)
0.86
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 2Homo sapiens (human)IC50 (µMol)0.06800.00290.46624.3000AID1183964
Metabotropic glutamate receptor 2Homo sapiens (human)Ki0.18000.00270.71586.4000AID1319703
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 2Homo sapiens (human)EC50 (µMol)0.91680.00061.17848.5000AID1183943; AID1319669; AID1319676; AID1319677; AID1319678; AID1319679; AID1319680; AID1319681; AID1319682
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)INH18.00000.10000.10000.1000AID1184033
Cytochrome P450 3A4Homo sapiens (human)INH18.00001.70002.85004.0000AID1184035
Cytochrome P450 2D6Homo sapiens (human)INH18.00003.20003.40003.6000AID1184034
Cytochrome P450 2C9 Homo sapiens (human)INH6.00004.40007.00009.1000AID1184036
5-hydroxytryptamine receptor 2AHomo sapiens (human)Kb1.10000.00060.16891.1000AID1184023
Cytochrome P450 2C19Homo sapiens (human)INH7.00007.00007.00007.0000AID1184037
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (95)

Processvia Protein(s)Taxonomy
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)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
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)
negative regulation of adenylate cyclase activityMetabotropic glutamate receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 2Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 2Homo sapiens (human)
gene expressionMetabotropic glutamate receptor 2Homo sapiens (human)
glutamate secretionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of glutamate secretionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of dopamine secretionMetabotropic glutamate receptor 2Homo sapiens (human)
behavioral response to nicotineMetabotropic glutamate receptor 2Homo sapiens (human)
response to cocaineMetabotropic glutamate receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionMetabotropic glutamate receptor 2Homo sapiens (human)
long-term synaptic depressionMetabotropic glutamate receptor 2Homo sapiens (human)
intracellular glutamate homeostasisMetabotropic glutamate receptor 2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of response to drugMetabotropic glutamate receptor 2Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (48)

Processvia Protein(s)Taxonomy
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)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
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)
G protein-coupled receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
calcium channel regulator activityMetabotropic glutamate receptor 2Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 2Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
scaffold protein bindingMetabotropic glutamate receptor 2Homo sapiens (human)
group II metabotropic glutamate receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
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)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
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 membraneMetabotropic glutamate receptor 2Homo sapiens (human)
axonMetabotropic glutamate receptor 2Homo sapiens (human)
dendriteMetabotropic glutamate receptor 2Homo sapiens (human)
presynaptic membraneMetabotropic glutamate receptor 2Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 2Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 2Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (155)

Assay IDTitleYearJournalArticle
AID1183943Positive allosteric modulation of human mGlu2 receptor expressed in CHO cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184023Antagonist activity at 5HT2A receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319678Positive allosteric modulation at human mGlu2 receptor F643A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184041Tmax in dog at 1 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183951AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183991Selectivity for human mGlu2 receptor over ETA receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319683Lipophilicity, log P of the compound2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183994Selectivity for human mGlu2 receptor over H2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183993Selectivity for human mGlu2 receptor over H1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183946Metabolic stability in rat liver microsomes assessed as compound metabolized at 5 uM after 15 mins by MS/MS analysis in presence of NADPH2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183961Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on deep sleep stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184000Selectivity for human mGlu2 receptor over MC4 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184048Therapeutic index, ratio of cardiotoxicity in anesthetized guinea pig to efficacy free concentration in Sprague-Dawley rat sleep-wake EEG paradigm model2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319688Fraction unbound in rat plasma assessed as free drug level at 5 uM by rapid equilibrium dialysis method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184047Therapeutic index, ratio of activity at rabbit purkinje fibre to efficacy free concentration in Sprague-Dawley rat sleep-wake EEG paradigm model2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184027Plasma protein binding in human2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183975Selectivity for human mGlu2 receptor over 5HT1A receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184029Plasma protein binding in mouse2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184031Apparent permeability from apical to basolateral side in human Caco2 cells2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184035Inhibition of human CYP3A4 (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319674Metabolic stability in rat liver microsomes assessed as compound metabolized at 5 uM measured after 15 mins2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184042Elimination half life in dog at 1 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319684Dissociation constant, pKa of the compound2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183987Selectivity for human mGlu2 receptor over CCR1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319703Displacement of [3H]8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-phenyl-1-piperidinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine from mGlu2 receptor (unknown origin)2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183989Selectivity for human mGlu2 receptor over D2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319676Positive allosteric modulation of wild-type human mGlu2 receptor expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183969Binding affinity to rat mGlu6 receptor expressed in CHO cells assessed as calcium mobilization by [35S]GTPgamma binding assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184036Inhibition of human CYP2C9 (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184032Apparent permeability from basolateral to apical side in human Caco2 cells2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183948Clearance in Sprague-Dawley rat at 2.5 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319699Tmax in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319685Solubility of the compound in water at pH 7.42016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184040Volume of distribution at steady state in dog at 1 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319689Fraction unbound in rat brain assessed as free drug level at 5 uM by rapid equilibrium dialysis method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319719Cmax in plasma of Sprague-Dawley rat sleep-wake EEG paradigm model as at 3 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183971Selectivity ratio of IC50 for human mGlu3 receptor to IC50 for human mGlu2 receptor2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319690Clearance in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184026Solubility of the compound in 20% HP-beta-CD at pH 42014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184034Inhibition of human CYP2D6 (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183984Selectivity for human mGlu2 receptor over beta1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184010Selectivity for human mGlu2 receptor over V1A receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184018Selectivity for human mGlu2 receptor over CICH receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184015Selectivity for human mGlu2 receptor over alpha2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183985Selectivity for human mGlu2 receptor over BK2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183944Positive allosteric modulation of human mGlu2 receptor expressed in CHO cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins relative to glutamate2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183962Dissociation constant, pKa of the compound2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319675Inhibition of human ERG expressed in HEK293 cells assessed as reduction in maximal tail current at 3 uM and holding potential of -60 mV measured after 5 mins by patch-clamp assay2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319697Clearance in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184051Genotoxicity in human TK6 cells up to 150 ug/ml by in vitro micronucleus test2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183958Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on passive wake stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183959Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on intermediate state at 3 mg/kg, po after 4 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183957Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on active wake stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319673Metabolic stability in human liver microsomes assessed as compound metabolized at 5 uM measured after 15 mins2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184039Clearance in dog at 1 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183956Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as reduction in REM sleep at 3 mg/kg, po after 4 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319680Positive allosteric modulation at human mGlu2 receptor N735D mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183968Binding affinity to human mGlu4 receptor expressed in rat L929 cells assessed as calcium mobilization by [35S]GTPgamma binding assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184043AUC (0 to infinity) in dog at 2.5 mg/kg, po2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183999Selectivity for human mGlu2 receptor over M3 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319691Elimination half life in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184016Selectivity for human mGlu2 receptor over BZD receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183979Selectivity for human mGlu2 receptor over 5HT7 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319677Positive allosteric modulation at human mGlu2 receptor L639A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183950Tmax in Sprague-Dawley rat at 2.5 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184038Volume of distribution at steady state in Sprague-Dawley rat at 2.5 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183986Selectivity for human mGlu2 receptor over CCKA receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183955Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat assessed effect on sleep-wake EEG paradigm after 20 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184003Selectivity for human mGlu2 receptor over NK3 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183949Elimination half life in Sprague-Dawley rat at 2.5 mg/kg, iv2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319702Oral bioavailability in Beagle dog at 5 mg/kg2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183996Selectivity for human mGlu2 receptor over CXCR2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183982Selectivity for human mGlu2 receptor over A3 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184019Selectivity for human mGlu2 receptor over GABA receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184045Oral bioavailability in dog at 2.5 mg/kg2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1607614Positive allosteric modulation of mGluR2 (unknown origin) relative to control2019Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases.
AID1184012Selectivity for human mGlu2 receptor over SST receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183967Binding affinity to human mGlu5 receptor expressed in HEK293 cells assessed as calcium mobilization by [35S]GTPgamma binding assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319671Kinetic solubility of the compound in 20% HP-beta-cyclodextrin at pH 4 by UPLC/UV method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319701Cmax in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319682Positive allosteric modulation at human mGlu2 receptor F776A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183976Selectivity for human mGlu2 receptor over 5HT3 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184001Selectivity for human mGlu2 receptor over NET (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184044Cmax in dog at 2.5 mg/kg, po2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319681Positive allosteric modulation at human mGlu2 receptor W773A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319695Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183953Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319700AUC (0 to infinity) in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184046Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat assessed free plasma drug level causing effect on sleep-wake EEG paradigm after 20 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184021Selectivity for human mGlu2 receptor over NaCH receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319698Half life in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319725Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat sleep-wake EEG paradigm model assessed as lowest active dose required to show effect on sleep-wake cycle by electroencephalogram analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183966Binding affinity to human mGlu3 receptor expressed in HEK293 cells assessed as calcium mobilization by [35S]GTPgamma binding assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183995Selectivity for human mGlu2 receptor over IL8B receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183952Cmax in Sprague-Dawley rat at 10 mg/kg, po2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183965Binding affinity to human mGlu1 receptor expressed in HEK293 cells assessed as calcium mobilization by [35S]GTPgamma binding assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184037Inhibition of human CYP2C19 (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183960Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on light sleep stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184024Selectivity for human mGlu2 receptor over 5HT2A receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183980Selectivity for human mGlu2 receptor over A1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319692Tmax in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184022Selectivity for human mGlu2 receptor over SKCaCH receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184013Selectivity for human mGlu2 receptor over 5HT1B receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319694Cmax in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319669Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184052Genotoxicity in human TK6 cells up to 150 ug/ml by in vitro micronucleus test in presence of rat liver S9 fraction2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319679Positive allosteric modulation at wild type human mGlu2 receptor L732A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect preincubated for 30 mins prior to glutamate challenge measured after 30 mins by [35S]GTP-gammaS bi2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1183945Metabolic stability in human liver microsomes assessed as compound metabolized at 5 uM after 15 mins by MS/MS analysis in presence of NADPH2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184011Selectivity for human mGlu2 receptor over VIP receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183997Selectivity for human mGlu2 receptor over M1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183974Selectivity ratio of IC50 for rat mGlu6 receptor to IC50 for human mGlu2 receptor2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183977Selectivity for human mGlu2 receptor over 5HT5A receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184008Selectivity for human mGlu2 receptor over OP3 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184006Selectivity for human mGlu2 receptor over NT1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184004Selectivity for human mGlu2 receptor over NPY1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184030Plasma protein binding in dog2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183990Selectivity for human mGlu2 receptor over DAT (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183988Selectivity for human mGlu2 receptor over D1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184020Selectivity for human mGlu2 receptor over KCH receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183964Displacement of [3H]19 from human mGlu2 receptor expressed in CHO cells2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184009Selectivity for human mGlu2 receptor over ORL1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183970Selectivity ratio of IC50 for human mGlu1 receptor to IC50 for human mGlu2 receptor2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184007Selectivity for human mGlu2 receptor over OP1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183983Selectivity for human mGlu2 receptor over AT1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184028Plasma protein binding in rat2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183981Selectivity for human mGlu2 receptor over A2A receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184025Solubility of the compound in water2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319696Ratio of drug level in brain to plasma of Swiss mouse at 10 mg/kg, sc measured after 1 hr2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184017Selectivity for human mGlu2 receptor over CaCH receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183973Selectivity ratio of IC50 for human mGlu4 receptor to IC50 for human mGlu2 receptor2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183954Ratio of drug level in brain to plasma in Swiss mouse at 10 mg/kg, sc after 1 hr2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319670Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method relat2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1319668Apparent permeability across apical to basolateral side over basolateral to apical side in human Caco2 cells at 1 uM measured after 120 mins2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184014Selectivity for human mGlu2 receptor over alpha1 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319726Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat sleep-wake EEG paradigm model assessed as plasma concentration required to show effect on sleep-wake cycle by electroencephalogram analysis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184002Selectivity for human mGlu2 receptor over NK2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183998Selectivity for human mGlu2 receptor over M2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319672Kinetic solubility of the compound at pH 7 by UPLC/UV method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184049Therapeutic index, ratio of cardiotoxicity in anesthetized dog to efficacy free concentration in Sprague-Dawley rat sleep-wake EEG paradigm model2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183972Selectivity ratio of IC50 for human mGlu5 receptor to IC50 for human mGlu2 receptor2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319686Solubility of the compound in water at pH 22016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184005Selectivity for human mGlu2 receptor over NPY2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183978Selectivity for human mGlu2 receptor over 5HT6 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183992Selectivity for human mGlu2 receptor over GAL2 receptor (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183963Lipophilicity, log P of the compound at pH 6.82014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1184050Mutagenic activity in Salmonella typhimurium TA98 assessed as reverse mutation up to 125 ug/ml by Ames test2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1319693AUC (0 to infinity) in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
AID1184033Inhibition of human CYP1A2 (unknown origin)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
AID1183947Inhibition of human ERG channel transfected in HEK293 cells at 3 uM by patch clamp technique2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.
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.
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.
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.
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.
AID1346271Human mGlu2 receptor (Metabotropic glutamate receptors)2015Pharmacology research & perspectives, Feb, Volume: 3, Issue:1
Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.
[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's9 (81.82)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.55

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 Index28.55 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index28.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.55)

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]