Page last updated: 2024-12-09

n-(3-chlorophenyl)picolinamide

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

Description

N-(3-chlorophenyl)picolinamide: a metabotropic glutamate receptor 4 (mGlu4) positive allosteric modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID836002
CHEMBL ID556667
SCHEMBL ID2530324
MeSH IDM0572454

Synonyms (35)

Synonym
VU0364770-1
n-(3-chlorophenyl)picolinamide
CHEMBL556667 ,
n-(3-chlorophenyl)pyridine-2-carboxamide
AKOS003020541
cid_836002
bdbm50293743
61350-00-3
vu0364770
S2862
gtpl6234
c12h9cln2o
SCHEMBL2530324
vu 0364770
n-(3-chlorophenyl)-2-pyridinecarboxamide
HB0640
AC-32759
CS-6072
HY-100588
EX-A1099
DTXSID00356877
HMS3651P19
SW219537-1
n-(3-chloro-phenyl)-pyridine-2-carboxamide
BCP19097
vu-0364770
mfcd00548412
Q27089187
HMS3884L20
CCG-266813
AS-56201
A913490
EN300-11595327
SY122460
bk0 ,

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" VU0364770 showed efficacy alone or when administered in combination with L-DOPA or an adenosine 2A (A2A) receptor antagonist currently in clinical development (preladenant)."( The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Amalric, M; Blobaum, AL; Bode, J; Bridges, TM; Bubser, M; Conn, PJ; Daniels, JS; Dickerson, JW; Engers, DW; Hopkins, CR; Italiano, K; Jadhav, S; Jones, CK; Lindsley, CW; Morrison, RD; Niswender, CM; Thompson, AD; Turle-Lorenzo, N, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor, metabotropic 4Homo sapiens (human)Potency0.00000.00000.00000.0000AID2180
metabotropic glutamate receptor 4 precursorRattus norvegicus (Norway rat)Potency0.00000.00000.00000.0000AID2179
[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)
Glutamate receptor, metabotropic 4Homo sapiens (human)EC50 (µMol)1.09000.23901.63483.4300AID2197
metabotropic glutamate receptor 6 precursorHomo sapiens (human)EC50 (µMol)1.25001.25001.25001.2500AID2191
metabotropic glutamate receptor 5 precursorRattus norvegicus (Norway rat)EC50 (µMol)1.24000.52300.52300.5230AID2199
metabotropic glutamate receptor 8 precursorRattus norvegicus (Norway rat)EC50 (µMol)9.14002.28002.28002.2800AID2181
metabotropic glutamate receptor 4 precursorRattus norvegicus (Norway rat)EC50 (µMol)0.44600.10700.33300.5970AID2183; AID2185
Cytochrome P450 2C9 Homo sapiens (human)EC50 (µMol)0.33000.00080.41702.3000AID1242926
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.47000.02700.87933.0000AID2188
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.47000.02700.97093.0000AID2188
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.47000.02700.97093.0000AID2188
Metabotropic glutamate receptor 4Rattus norvegicus (Norway rat)EC50 (µMol)0.31000.00902.54409.4900AID1242926; AID420537
Metabotropic glutamate receptor 4Homo sapiens (human)EC50 (µMol)1.12400.00401.71939.8000AID1242925; AID1397000; AID1873141; AID420542
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
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)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 4Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 4Homo sapiens (human)
neurotransmitter secretionMetabotropic glutamate receptor 4Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 4Homo sapiens (human)
regulation of neuron apoptotic processMetabotropic glutamate receptor 4Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 4Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
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)
G protein-coupled receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
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)
plasma membraneMetabotropic glutamate receptor 4Rattus norvegicus (Norway rat)
plasma membraneMetabotropic glutamate receptor 4Homo sapiens (human)
cytoplasmic vesicleMetabotropic glutamate receptor 4Homo sapiens (human)
presynapseMetabotropic glutamate receptor 4Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1346283Rat mGlu4 receptor (Metabotropic glutamate receptors)2012The Journal of pharmacology and experimental therapeutics, Feb, Volume: 340, Issue:2
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
AID1346285Human mGlu4 receptor (Metabotropic glutamate receptors)2012The Journal of pharmacology and experimental therapeutics, Feb, Volume: 340, Issue:2
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
AID420543Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization relative to glutamate2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
AID1873141Agonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
AID420545Activity at human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as fold shifting of glutamate-induced response to left at 30 uM2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
AID420546Activity at rat mGluR4 expressed in HEK293 cells coexpressing Gqi5 protein assessed as fold shifting of glutamate-induced response to left at 30 uM2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
AID420542Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
AID420537Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
AID1397000Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay2018Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu
AID1242926Positive allosteric modulator activity at rat mGlu4 receptor2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.
AID420544Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux relative to glutamate2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
AID1242925Positive allosteric modulator activity at human mGlu4 receptor2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's4 (66.67)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.18

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index13.18 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index5.12 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]