Page last updated: 2024-12-10

4-[3-(4-fluorophenyl)-2-methyl-7-oxo-1H-pyrazolo[1,5-a]pyrimidin-5-yl]-1-piperidinecarboxylic acid ethyl ester

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Cross-References

ID SourceID
PubMed CID5308428
CHEMBL ID1496110
CHEBI ID108309
SCHEMBL ID17682780

Synonyms (17)

Synonym
MLS000116905 ,
smr000093859
CHEBI:108309
ethyl 4-[3-(4-fluorophenyl)-2-methyl-7-oxo-1h-pyrazolo[1,5-a]pyrimidin-5-yl]piperidine-1-carboxylate
901715-05-7
trpc6-in-1
AKOS004916430
HMS2249I17
CHEMBL1496110
Q27187013
4-[3-(4-fluorophenyl)-2-methyl-7-oxo-1h-pyrazolo[1,5-a]pyrimidin-5-yl]-1-piperidinecarboxylic acid ethyl ester
SR-01000095877-1
sr-01000095877
SCHEMBL17682780
HY-101547
CS-0021690
MS-26735
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
pyrazoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (26)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency13.55710.044717.8581100.0000AID485294; AID485341
Chain A, HADH2 proteinHomo sapiens (human)Potency19.95260.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency19.95260.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency14.58100.004110.890331.5287AID504466
TDP1 proteinHomo sapiens (human)Potency5.28600.000811.382244.6684AID686978; AID686979
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency17.78280.707912.194339.8107AID720542
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency7.94330.28189.721235.4813AID2326
67.9K proteinVaccinia virusPotency20.81140.00018.4406100.0000AID720579; AID720580
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency14.21910.316212.443531.6228AID902; AID924
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency35.48130.001815.663839.8107AID894
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency11.58210.00419.984825.9290AID504444
huntingtin isoform 2Homo sapiens (human)Potency11.22020.000618.41981,122.0200AID1688
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency28.18380.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency28.18380.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency28.18380.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.29470.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency20.59620.004611.374133.4983AID624297
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
Integrin beta-3Homo sapiens (human)Potency15.84890.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency15.84890.316211.415731.6228AID924
[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)
Short transient receptor potential channel 3Homo sapiens (human)EC50 (µMol)0.45000.45000.45000.4500AID1447372
Short transient receptor potential channel 6Mus musculus (house mouse)EC50 (µMol)3.94001.40003.94007.2000AID1447370; AID1447381; AID1447394; AID1447397
Short transient receptor potential channel 7Homo sapiens (human)EC50 (µMol)0.81350.49700.81351.1300AID1447383; AID1447402
Short transient receptor potential channel 4 Mus musculus (house mouse)EC50 (µMol)4.70004.70004.70004.7000AID1578756
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (79)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
calcium ion transportShort transient receptor potential channel 3Homo sapiens (human)
phototransductionShort transient receptor potential channel 3Homo sapiens (human)
positive regulation of calcium ion transport into cytosolShort transient receptor potential channel 3Homo sapiens (human)
response to ATPShort transient receptor potential channel 3Homo sapiens (human)
response to calcium ionShort transient receptor potential channel 3Homo sapiens (human)
calcium ion transmembrane transportShort transient receptor potential channel 3Homo sapiens (human)
positive regulation of cardiac muscle hypertrophy in response to stressShort transient receptor potential channel 3Homo sapiens (human)
single fertilizationShort transient receptor potential channel 3Homo sapiens (human)
regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 3Homo sapiens (human)
calcium ion transmembrane transportShort transient receptor potential channel 7Homo sapiens (human)
regulation of cytosolic calcium ion concentrationShort transient receptor potential channel 7Homo sapiens (human)
single fertilizationShort transient receptor potential channel 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (25)

Processvia Protein(s)Taxonomy
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
calcium-activated cation channel activityShort transient receptor potential channel 3Homo sapiens (human)
calcium channel activityShort transient receptor potential channel 3Homo sapiens (human)
protein bindingShort transient receptor potential channel 3Homo sapiens (human)
metal ion bindingShort transient receptor potential channel 3Homo sapiens (human)
inositol 1,4,5 trisphosphate bindingShort transient receptor potential channel 3Homo sapiens (human)
store-operated calcium channel activityShort transient receptor potential channel 3Homo sapiens (human)
calcium channel activityShort transient receptor potential channel 7Homo sapiens (human)
protein bindingShort transient receptor potential channel 7Homo sapiens (human)
inositol 1,4,5 trisphosphate bindingShort transient receptor potential channel 7Homo sapiens (human)
store-operated calcium channel activityShort transient receptor potential channel 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Processvia Protein(s)Taxonomy
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
plasma membraneShort transient receptor potential channel 3Homo sapiens (human)
cation channel complexShort transient receptor potential channel 3Homo sapiens (human)
plasma membraneShort transient receptor potential channel 3Homo sapiens (human)
nuclear envelopeShort transient receptor potential channel 7Homo sapiens (human)
plasma membraneShort transient receptor potential channel 7Homo sapiens (human)
perinuclear region of cytoplasmShort transient receptor potential channel 7Homo sapiens (human)
plasma membraneShort transient receptor potential channel 7Homo sapiens (human)
cation channel complexShort transient receptor potential channel 7Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
AID1745847CMV-Luciferase Counterscreen for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745849Viability Counterscreen for CMV-Luciferase Assay of Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745846Firefly Luciferase Counterscreen for Inhibitors of ATXN expression
AID1745850Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression
AID1745848Confirmatory qHTS for Inhibitors of ATXN expression
AID1447403Antagonist activity at human TRPC7 receptor expressed in HEK293 cells assessed as channel desensitization up to 30 uM in presence of 0.1 mM Ca2+ by whole cell patch-clamp method2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1578756Agonist activity at mouse TRPC4 expressed in HEK293 cells coexpressing M5 receptor assessed as induction of TRPC4-mediated calcium influx by fluorescence method2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
AID1447397Agonist activity at mouse TRPC6 expressed in HEK293 cells co-expressing Gq11-PLCbeta fused M5 receptor assessed as increase in intracellular calcium level by Fluo-4-AM dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447388Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in intracellular calcium level at 33 uM measured for 2.5 mins by Fluo-8-AM dye based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447402Agonist activity at human TRPC7 receptor expressed in HEK293 cells assessed as induction of channel current in presence of 0.1 mM Ca2+ by whole cell patch-clamp method2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447375Inhibition of mouse TRPM8 expressed in HEK293 cells assessed as decrease in methanol-evoked increase in intracellular calcium level at 22 uM preincubated for 2 mins followed by methanol addition measured for 2.5 mins by Fluo8-AM dye-based fluorescence ass2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447372Agonist activity at human TRPC3 expressed in HEK293 cells assessed as induction of membrane depolarization measured for 2.5 mins in presence of 0.5 mM Ca2+ by FLIPR membrane potential dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447392Agonist activity at human TRPM5 expressed in HEK293 cells assessed as induction of membrane depolarization at 33 uM measured for 2.5 mins by FLIPR membrane potential dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447386Agonist activity at human TRPC5 expressed in HEK293 cells assessed as induction of membrane depolarization at 33 uM measured for 2.5 mins by FLIPR membrane potential dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447373Agonist activity at human TRPC3 expressed in HEK293 cells assessed as increase in intracellular calcium level measured for 2.5 mins by Fluo-8-AM dye based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447382Agonist activity at human TRPC7 expressed in HEK293 cells assessed as increase in membrane depolarization measured for 2.5 mins in presence of 2 mM Ca2+ by FLIPR membrane potential dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447394Agonist activity at mouse TRPC6 expressed in HEK293 cells co-expressing Gq11-PLCbeta fused M5 receptor assessed as induction of membrane potential depolarization measured for 2.5 mins by FLIPR assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447383Agonist activity at human TRPC7 expressed in HEK293 cells assessed as increase in intracellular calcium level measured for 2.5 mins in presence of 2 mM Ca2+ by Fluo8-AM dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447391Agonist activity at human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level at 33 uM measured for 2.5 mins by Fluo-8-AM dye based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447396Induction of intracellular calcium level in HEK293 cells at 30 uM measured for 2.5 mins by Fluo-4-AM dye based FLIPR assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447381Agonist activity at mouse TRPC6 expressed in HEK293 cells co-expressing Gq11-PLCbeta fused M5 receptor assessed as peak current changes at +80 mV by whole cell patch-clamp method2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447389Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level at 33 uM measured for 2.5 mins by Fluo-8-AM dye based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447370Agonist activity at mouse TRPC6 expressed in HEK293 cells co-expressing Gq11-PLCbeta fused M5 receptor assessed as increase in intracellular calcium level measured for 2.5 mins by Fluo-8-AM dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447401Agonist activity at human TRPC3 expressed in HEK293 cells assessed as induction of channel current at 10 uM measured for 2.5 mins in presence of 0.5 mM Ca2+ by whole cell patch-clamp method2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447385Agonist activity at mouse TRPC4beta expressed in HEK293 cells co-expressing MOR assessed as induction of membrane depolarization at 33 uM measured for 2.5 mins by FLIPR membrane potential dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447400Agonist activity at human TRPC3 expressed in HEK293 cells assessed as induction of membrane depolarization measured for 2.5 mins in presence of 2 mM Ca2+ by FLIPR membrane potential dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447399Antagonist activity at mouse TRPC6 expressed in HEK293 cells co-expressing Gq11-PLCbeta fused M5 receptor assessed as channel desensitization at 20 to 100 uM at +80 mV in presence of 0.1 mM Ca2+ by whole cell patch-clamp method2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447390Agonist activity at mouse TRPV3 expressed in HEK293 cells assessed as increase in intracellular calcium level at 33 uM measured for 2.5 mins by Fluo-8-AM dye based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447387Agonist activity at mouse TRPM8 expressed in HEK293 cells assessed as increase in intracellular calcium level at 33 uM measured for 2.5 mins by Fluo-8-AM dye based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447371Antagonist activity at mouse TRPC4beta expressed in HEK293 cells co-expressing MOR decrease in DAMGO-evoked intracellular calcium level by Fluo-8-AM dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447398Agonist activity at mouse TRPC4beta expressed in HEK293 cells co-expressing MOR assessed as increase in intracellular calcium level at 33 uM measured for 2.5 mins by Fluo-8-AM dye-based fluorescence assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
AID1447395Induction of membrane potential depolarization in HEK293 cells measured for 2.5 mins by FLIPR assay2017Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11
Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's5 (71.43)24.3611
2020's1 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.29

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 Index12.29 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]