Page last updated: 2024-12-07

5-(4-piperidyl)isoxazol-3-ol

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

Description

5-(4-piperidyl)isoxazol-3-ol: structure given in first source; a partial agonist at the GABA-A receptor on cultured hippocampal neurones; antagonizes muscimol-stimulated benzodiazepine binding to rat cortical membranes [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID125520
CHEMBL ID311761
CHEBI ID34433
SCHEMBL ID1656142
SCHEMBL ID13406229
MeSH IDM0197530

Synonyms (26)

Synonym
chebi:34433 ,
CHEMBL311761 ,
5-(piperidin-4-yl)isoxazol-3-ol
bdbm50032954
5-piperidin-4-yl-isoxazol-3-ol
5-piperidin-4-yl-isoxazol-3-ol(4-piol)
4-piol
C13710 ,
5-(4-piperidyl)isoxazol-3-ol
132033-91-1
ZINC20272675 ,
AC1L2OPK ,
5-piperidin-4-yl-1,2-oxazol-3-one
AKOS002272847
STL229598
5-(piperidin-4-yl)-1,2-oxazol-3-ol
3(2h)-isoxazolone, 5-(4-piperidinyl)-
SCHEMBL1656142
SCHEMBL13406229
5-(4-piperidyl)isoxazol-3-one
DTXSID70157318
5-(4-piperidyl)-3-isoxazolol
Q27116061
3(2h)-isoxazolone,5-(4-piperidinyl)-(9ci)
PD121069
EN300-1709473

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" 4-PIOL antagonized the response to isoguvacine with a parallel shift to the right of the dose-response curve."( Electrophysiological studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones.
Falch, E; Kristiansen, U; Krogsgaard-Larsen, P; Lambert, JD, 1991
)
0.28
"44 μM, no detectable activity against GABAa, and with DMPK properties leading to a predicted dose of 340 mg twice a day oral dosing in humans."( Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
Boström, J; Cheng, L; Evertsson, E; Fex, T; Gustafsson, D; Hilgendorf, C; Jonforsen, M; Karle, M; Larsson, LO; Lindberg, W; Ohlsson, B; Pahlén, S; Pettersen, D; Plowright, AT; Schell, P; Thelin, A; Wahlund, G; Xue, Y, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperidines
[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 (23)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00001.01016.8100AID71392
PlasminogenHomo sapiens (human)IC50 (µMol)2.80000.02503.628010.0000AID1154948; AID728964
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50 (µMol)500.59350.00011.14948.0000AID472676
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki11.00000.00000.21085.6234AID281444
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50 (µMol)500.59350.00011.29158.0000AID472676
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki11.00000.00000.18819.0000AID281444
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.505710.0000AID71975
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki9.10000.00020.561410.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.497310.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki9.10000.00020.635210.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki9.10000.00020.621710.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.498810.0000AID71975
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki9.10000.00020.675810.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.504610.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki9.10000.00020.646910.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki11.00000.00010.20769.0000AID281444
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki9.10000.00020.671210.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50 (µMol)500.59350.00010.93746.0000AID472676
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.506510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki9.10000.00020.557710.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.505710.0000AID71975
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki9.10000.00020.640310.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki9.10000.00020.570810.0000AID239462; AID72135
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
GABA theta subunitRattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)110.00000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki9.10000.00020.656110.0000AID239462; AID72135
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00001.05326.8100AID71392
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (34)

Processvia Protein(s)Taxonomy
proteolysisPlasminogenHomo sapiens (human)
blood coagulationPlasminogenHomo sapiens (human)
negative regulation of cell population proliferationPlasminogenHomo sapiens (human)
negative regulation of cell-substrate adhesionPlasminogenHomo sapiens (human)
extracellular matrix disassemblyPlasminogenHomo sapiens (human)
tissue regenerationPlasminogenHomo sapiens (human)
fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationPlasminogenHomo sapiens (human)
myoblast differentiationPlasminogenHomo sapiens (human)
muscle cell cellular homeostasisPlasminogenHomo sapiens (human)
tissue remodelingPlasminogenHomo sapiens (human)
biological process involved in interaction with symbiontPlasminogenHomo sapiens (human)
negative regulation of fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of fibrinolysisPlasminogenHomo sapiens (human)
trophoblast giant cell differentiationPlasminogenHomo sapiens (human)
labyrinthine layer blood vessel developmentPlasminogenHomo sapiens (human)
mononuclear cell migrationPlasminogenHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionPlasminogenHomo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherinPlasminogenHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
roof of mouth developmentGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
protease bindingPlasminogenHomo sapiens (human)
endopeptidase activityPlasminogenHomo sapiens (human)
serine-type endopeptidase activityPlasminogenHomo sapiens (human)
signaling receptor bindingPlasminogenHomo sapiens (human)
protein bindingPlasminogenHomo sapiens (human)
serine-type peptidase activityPlasminogenHomo sapiens (human)
enzyme bindingPlasminogenHomo sapiens (human)
kinase bindingPlasminogenHomo sapiens (human)
protein domain specific bindingPlasminogenHomo sapiens (human)
apolipoprotein bindingPlasminogenHomo sapiens (human)
protein-folding chaperone bindingPlasminogenHomo sapiens (human)
protein antigen bindingPlasminogenHomo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
identical protein bindingGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extracellular regionPlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
plasma membranePlasminogenHomo sapiens (human)
external side of plasma membranePlasminogenHomo sapiens (human)
cell surfacePlasminogenHomo sapiens (human)
platelet alpha granule lumenPlasminogenHomo sapiens (human)
collagen-containing extracellular matrixPlasminogenHomo sapiens (human)
extracellular exosomePlasminogenHomo sapiens (human)
blood microparticlePlasminogenHomo sapiens (human)
Schaffer collateral - CA1 synapsePlasminogenHomo sapiens (human)
glutamatergic synapsePlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID1154951Apparent permeability across apical to basolateral side in human Caco2 cells2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
AID25820PKa values of the compound1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID728958Lipophilicity, log D of the compound2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID71822Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID1154950Displacement of [3H]-muscimol from GABAA receptor in Sprague-Dawley rat brain membranes after 1 hr by microbeta scintillation counting analysis2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
AID472677Displacement of [3H]muscimol from GABAA in rat synaptic membrane by scintillation counting2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.
AID71386Affinity for GABA-B receptor by inhibiting GABA uptake into rat brain synaptosomes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID239462Displacement of [3H]muscimol from rat brain gamma-aminobutyric-acid GABA-A receptor2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID1154948Binding affinity to human full length Glu-plasminogen in buffer assessed as inhibition of interaction with fibrin preincubated for 15 mins followed by thrombin addition measured every 2 mins for 15 hrs by Spectra-Max reader analysis in presence of tPA2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
AID1154949Binding affinity to full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin in presence of tPA2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
AID728960Ratio of TXA IC50 to compound IC50 for plasminogen/fibrinogen interaction in human platelet-poor plasma by microtiter plate analysis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID71975Inhibition of Gamma-aminobutyric acid A (GABA-A) receptor in vitro by whole-cell patch-clamp recording in cultured cerebral cortical neurones2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
AID132660Electrophysiology using Whole-cell patch-clamp recordings in mouse embryos2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID196024Concentration inhibiting GABA uptake rat brain synaptosomes.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID281443Displacement of [3H]GABA from GABAB receptor in Sprague-Dawley rat brain synaptic membrane at 100 uM2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
AID72457Affinity for GABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID472676Agonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells at < 500 uM by FMP red assay2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.
AID1154976Potency index, ratio of tranexamic acid IC50 to compound IC50 for full length human Glu-plasminogen in buffer assessed as inhibition of interaction with fibrin2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
AID71392Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID728963Dissociation constant, pKa of the compound at acidic pH by pressure-assisted capillary electrophoresis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID248086In vitro concentration required to inhibit peak currents in cerebral cortical neurones of rat2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
AID728962Dissociation constant, pKa of the compound at basic pH by pressure-assisted capillary electrophoresis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID72135In vitro inhibition of [3H]muscimol to rat brain synaptic membranes2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
AID728961Apparent permeability from apical to basolateral side in human Caco2 cells at pH 6.5 by LC/MS analysis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID728965Inhibition of plasminogen/fibrinogen interaction in pooled citreated human platelet-poor plasma assessed as inhibition of lysis of CaCl2/t-PA-induced clot by microtiter plate analysis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID728959Ratio of TXA IC50 to compound IC50 for human Glu-plasminogen/fibrinogen interaction by clot-lysis buffer assay2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID235130Reversal potential is determined electrophysiologically against the GABA A receptor1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
AID281444Antagonist activity at human GABAA alpha-1-beta-3-gamma-2S expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
AID728964Inhibition of human Glu-plasminogen/fibrinogen interaction in HEPES buffer assessed as inhibition of lysis of thrombin-induced clot preincubated for 15 mins prior to thrombin addition measured for 15 hrs by clot-lysis buffer assay2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid.
AID281442Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat brain synaptic membrane2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
AID1154977Potency index, ratio of tranexamic acid IC50 to compound IC50 for full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (23.81)18.2507
2000's11 (52.38)29.6817
2010's5 (23.81)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.33

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 Index11.33 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]