Page last updated: 2024-11-11

ubp 302

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Cross-References

ID SourceID
PubMed CID6420161
CHEMBL ID372797
SCHEMBL ID2265710
MeSH IDM0540034

Synonyms (36)

Synonym
(s)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrimidine-2,4-dione
UBC ,
NCGC00025352-01
tocris-2079
2F35
CHEMBL372797 ,
ubp-302
bdbm50178136
(s)-2-((3-(2-amino-2-carboxyethyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6h)-yl)methyl)benzoic acid
(s)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)-pyrimidine-2,4-dione
745055-91-8
ubp302
2-({3-[(2s)-2-amino-2-carboxyethyl]-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-1-yl}methyl)benzoic acid
gtpl4333
ubp 302
SCHEMBL2265710
DTXSID80423571
AKOS024456932
c15h15n3o6
ubp-296
SR-01000597533-1
sr-01000597533
ubp302, >=98% (hplc)
2-({3-[(2s)-2-amino-2-carboxyethyl]-2,6-dioxo-3,6-dihydropyrimidin-1(2h)-yl}methyl)benzoic acid
HMS3677E11
HMS3413E11
Q7863873
CS-0028945
HY-107604
2-[[3-[(2s)-2-amino-2-carboxyethyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid
MS-25018
2-((3-((2s)-2-azanyl-3-oxidanyl-3-oxidanylidene-propyl)-2,6-bis(oxidanylidene)pyrimidin-1-yl)methyl)benzoic acid
fz8ap4ua5y ,
HB0627
1(2h)-pyrimidinepropanoic acid, alpha-amino-3-[(2-carboxyphenyl)methyl]-3,4-dihydro-2,4-dioxo-, (alphas)-
(alphas)-alpha-amino-3-[(2-carboxyphenyl)methyl]-3,4-dihydro-2,4-dioxo-1(2h)-pyrimidinepropanoic acid
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency19.90540.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
phosphopantetheinyl transferaseBacillus subtilisPotency56.23410.141337.9142100.0000AID1490
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency19.95260.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.10000.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency6.30960.00636.904339.8107AID883
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency6.30960.00638.235039.8107AID883
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)106.00000.00011.617910.0000AID257196; AID262621
Glutamate receptor 1Rattus norvegicus (Norway rat)Ki117.00000.00000.41052.7800AID272848
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)106.00000.00011.700010.0000AID257196; AID262621
Glutamate receptor 2Rattus norvegicus (Norway rat)Ki117.00000.00000.68536.3000AID272848
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)106.00000.00011.700010.0000AID257196; AID262621
Glutamate receptor 3Rattus norvegicus (Norway rat)Ki117.00000.00000.71777.4000AID272848
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50 (µMol)106.00000.00011.700010.0000AID257196; AID262621
Glutamate receptor 4Rattus norvegicus (Norway rat)Ki117.00000.00000.52773.5700AID272848
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)Ki1,000.00000.00370.80254.1000AID257202; AID262622
Glutamate receptor 2Homo sapiens (human)IC50 (µMol)300.00000.01901.64035.5000AID281129
Glutamate receptor ionotropic, kainate 2Homo sapiens (human)IC50 (µMol)300.00000.07700.07700.0770AID281133
Glutamate receptor ionotropic, kainate 3Homo sapiens (human)IC50 (µMol)4.00000.07702.03854.0000AID1325321
[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)
Chain A, Glutamate Receptor, Ionotropic Kainate 1Rattus norvegicus (Norway rat)Kd3.94000.13002.03503.9400AID977611
Chain A, Glutamate Receptor, Ionotropic Kainate 1Rattus norvegicus (Norway rat)Kd3.94000.13002.03503.9400AID977611
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)Kd1.58130.01801.27203.9400AID257198; AID281120; AID450961
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)Kd0.40200.40201.09101.7800AID262620
[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)
Glutamate receptor ionotropic, kainate 1Homo sapiens (human)Kb0.80000.00800.40301.0000AID281130; AID281131
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (34)

Processvia Protein(s)Taxonomy
glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
nervous system developmentGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
central nervous system developmentGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
signal transductionGlutamate receptor 2Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor 2Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 2Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 2Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 2Homo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor 2Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 2Homo sapiens (human)
behavioral fear responseGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
intracellular calcium ion homeostasisGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
neuronal action potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
receptor clusteringGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
negative regulation of neuron apoptotic processGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
positive regulation of neuron apoptotic processGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
regulation of JNK cascadeGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
regulation of long-term neuronal synaptic plasticityGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
regulation of short-term neuronal synaptic plasticityGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
positive regulation of synaptic transmissionGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
neuron apoptotic processGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
inhibitory postsynaptic potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
modulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
detection of cold stimulus involved in thermoceptionGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
regulation of membrane potentialGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
regulation of membrane potentialGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
glutamate-gated receptor activityGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
kainate selective glutamate receptor activityGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 2Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 2Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 2Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 2Homo sapiens (human)
protein bindingGlutamate receptor 2Homo sapiens (human)
ligand-gated monoatomic cation channel activityGlutamate receptor 2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 2Homo sapiens (human)
SNARE bindingGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
extracellularly glutamate-gated ion channel activityGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
kainate selective glutamate receptor activityGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
PDZ domain bindingGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
ubiquitin conjugating enzyme bindingGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
ubiquitin protein ligase bindingGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
identical protein bindingGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
scaffold protein bindingGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
glutamate receptor activityGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
kainate selective glutamate receptor activityGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
intracellular membrane-bounded organelleGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
kainate selective glutamate receptor complexGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
presynaptic membraneGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, kainate 1Homo sapiens (human)
plasma membraneGlutamate receptor 2Homo sapiens (human)
external side of plasma membraneGlutamate receptor 2Homo sapiens (human)
postsynaptic densityGlutamate receptor 2Homo sapiens (human)
dendriteGlutamate receptor 2Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 2Homo sapiens (human)
asymmetric synapseGlutamate receptor 2Homo sapiens (human)
neuronal cell bodyGlutamate receptor 2Homo sapiens (human)
dendritic spineGlutamate receptor 2Homo sapiens (human)
excitatory synapseGlutamate receptor 2Homo sapiens (human)
postsynapseGlutamate receptor 2Homo sapiens (human)
postsynaptic endocytic zoneGlutamate receptor 2Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 2Homo sapiens (human)
plasma membraneGlutamate receptor 2Homo sapiens (human)
dendritic spineGlutamate receptor 2Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 2Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
dendrite cytoplasmGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
terminal boutonGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
perikaryonGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
mossy fiber rosetteGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
kainate selective glutamate receptor complexGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
presynaptic membraneGlutamate receptor ionotropic, kainate 2Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
axonGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
dendriteGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
dendrite cytoplasmGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
terminal boutonGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
perikaryonGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
kainate selective glutamate receptor complexGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
presynaptic membraneGlutamate receptor ionotropic, kainate 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC 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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID281132Antagonist activity at human recombinant GLUK5/GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID257198Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal rat dorsal root C-fibers2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
AID1325321Antagonist activity at recombinant GluK3 receptor (unknown origin) expressed in Xenopus oocyte assessed as inhibition of glutamate-induced current amplitude by voltage-clamp method2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands.
AID450957Displacement of [3H]CGP39653 from NMDA receptor in rat cortical membrane2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID257202Displacement of [3H]kainate from rat GLUK6 receptor expressed in HEK293 cells2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
AID450958Displacement of [3H]SYM2081 from rat recombinant iGluR6 expressed in baculovirus-infected insect Sf9 cells2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID281134Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID257201Displacement of [3H]SYM2081 from kainate receptor in rat brain membrane2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
AID272852Displacement of [3H]glycine from Gly/NMDA receptor in rat cortical synaptic membrane at 100 uM2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
AID450960Displacement of [3H]AMPA from wild type rat GluR2 S1S2 ligand binding core2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID1325314Displacement of [3H]-kainate from kainate receptor in rat brain membranes after 60 mins2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands.
AID450955Displacement of [3H]SYM2081 from rat recombinant iGluR5-1b expressed in baculovirus-infected insect Sf9 cells2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID262621Antagonist activity against AMPA receptor expressed in motoneurones by inhibition of fDR-VRP in the neonatal rat spinal cord2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
AID262620Antagonist activity against GLUK5-containing kainate receptor by inhibition of kainate-induced depolarization of neonatal rat dorsal root fibers2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
AID281120Activity at native GLUK5 kainate receptor assessed as antagonism of kainite-induced depolarization of neonatal anaesthetised rat dorsal root fibres2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID450956Displacement of [3H]kainic acid from kainate receptor in rat cortical membrane2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID272850Displacement of [3H]KA from high affinity KA receptor in rat cortical membrane2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
AID257200Displacement of [3H](S)-5-fluorowillardiine from AMPA receptor in rat brain membrane2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
AID262622Displacement of [3H]kainate from rat GLUK6 expressed in HEK293 cells2006Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
AID281129Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID257196Antagonist activity on AMPA receptor expressed on rat motoneurons by its ability to reduce the fast component dorsal root evoked ventral root potential (fDR-VRP)2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
AID281133Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID450961Displacement of [3H]S-glutamate from rat GluR5 S1S2 ligand binding core expressed in Escherichia coli (DE3)2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID450954Displacement of [3H]AMPA from AMPA receptor in rat cortical membrane2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID450959Displacement of [3H]SYM2081 from rat recombinant iGluR7A expressed in baculovirus-infected insect Sf9 cells2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
AID1325313Displacement of [3H]-AMPA from AMPA receptor in rat brain membranes after 30 mins2016Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22
Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands.
AID272848Displacement of [3H]AMPA from AMPA receptor in rat cortical synaptic membrane2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
AID281122Antagonist activity at native AMPA receptor assessed as fDR-VRP reduction of neonatal rat spinal cord motorneurones2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID272856Displacement of [3H]KA from low affinity KA receptor in rat cortical membrane2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
AID281131Antagonist activity at human recombinant GLUK5/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID281130Antagonist activity at human recombinant GLUK5 receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay2007Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2006The Journal of neuroscience : the official journal of the Society for Neuroscience, Mar-15, Volume: 26, Issue:11
Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (66.67)29.6817
2010's1 (11.11)24.3611
2020's2 (22.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]