Page last updated: 2024-11-12

pwz-029

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

Description

PWZ-029: a compound with moderate inverse agonist functional selectivity at GABA(A) receptors containing alpha5 subunits, improves passive, but not active, avoidance learning in rats; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9971547
CHEMBL ID45346
SCHEMBL ID6847260
MeSH IDM0525452

Synonyms (16)

Synonym
8-chloro-3-methoxymethyl-5-methyl-4,5-dihydro-2,5,10b-triaza-benzo[e]azulen-6-one
bdbm50034820
cid 9971547
pwz-029
CHEMBL45346 ,
SCHEMBL6847260
8-chloro-3-(methoxymethyl)-5-methyl-4h-imidazo[1,5-a][1,4]benzodiazepin-6-one
Q7121197
164025-33-6
8-chloro-4,5-dihydro-3-(methoxymethyl)-5-methyl-6h-imidazo(1,5-a)(1,4)benzodiazepin-6-one
6h-imidazo(1,5-a)(1,4)benzodiazepin-6-one, 8-chloro-4,5-dihydro-3-(methoxymethyl)-5-methyl-
unii-9d3ds54ycd
9D3DS54YCD ,
DTXSID801028421
8-chloro-3-(methoxymethyl)-5-methyl-4,5-dihydro-6h-imidazo[1,5-a][1,4]benzodiazepin-6-one
AKOS040753659
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (24)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.43640.00000.21085.6234AID1604529; AID219794; AID343402; AID533778; AID72927
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.71380.00000.18819.0000AID219794; AID219940; AID219954; AID343093; AID343095; AID343096; AID343402; AID343403; AID533778; AID533779; AID533780; AID533781; AID533782; AID71266; AID71268; AID72927; AID73089; AID73244; AID73523; AID73530
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.505710.0000AID71699
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki1.00000.00020.561410.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.497310.0000AID71699
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki1.00000.00020.635210.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki1.00000.00020.621710.0000AID72132
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.498810.0000AID71699
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki1.00000.00020.675810.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.504610.0000AID71699
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki1.00000.00020.646910.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.71380.00010.20769.0000AID219794; AID219940; AID219954; AID343093; AID343095; AID343096; AID343402; AID343403; AID533778; AID533779; AID533780; AID533781; AID533782; AID71266; AID71268; AID72927; AID73089; AID73244; AID73523; AID73530
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki1.00000.00020.671210.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.08450.00010.24425.6234AID1604531; AID343403; AID533782; AID73523; AID73530
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.30560.00010.25155.6234AID1604530; AID219954; AID343094; AID533780; AID73244
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.27600.00010.24015.6234AID1604528; AID219940; AID343093; AID533779; AID73089
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)Ki0.16940.00020.37095.6234AID343095; AID533781
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.506510.0000AID71699
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki1.00000.00020.557710.0000AID72132
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.505710.0000AID71699
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki1.00000.00020.640310.0000AID72132
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki1.00000.00020.570810.0000AID72132
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki3.20000.00020.41199.0000AID343096; AID71266; AID71268
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
GABA theta subunitRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.51400.00010.507510.0000AID71699
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki1.00000.00020.656110.0000AID72132
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
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)
behavioral fear responseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
associative learningGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
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-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signaling receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
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)
nucleoplasmGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cytosolGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuronal cell body membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
cerebellar Golgi cell to granule cell synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID343109Activity at GABAA alpha-3-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as potentiation of GABA-induced chloride current at 1 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID1604585Negative allosteric modulation of GABA-A alpha1 (unknown origin) assessed as reduction in DMCM induced current relative to control
AID1604591Selectivity ratio of Ki for binding affinity to GABAA alpha3beta3gamma2 (unknown origin) to Ki for binding affinity to GABAA alpha5beta3gamma2 (unknown origin)
AID343107Activity at GABAA alpha-4-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as potentiation of GABA-induced chloride current at 1 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID71268Binding affinity against Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-21998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via compar
AID219794Binding affinity against alpha-1-beta-3-gamma-2 GABAA/BzR receptor subtype.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via compar
AID343096Binding affinity to GABAA alpha-6-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343094Binding affinity to GABAA alpha-3-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID1604600Negative allosteric modulation of GABAA alpha5beta3gamma2 (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current response at -60 mV holding potential by two electrode voltage clamp method relative to control
AID343103Selectivity for GABAA alpha-5-beta-3-gamma-2 receptor over GABAA alpha-6-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343093Binding affinity to GABAA alpha-2-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID73523Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-22000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
AID533782Binding affinity to human recombinant GABA alpha-5-beta-3-gamma-2 receptor2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
The GABA(A) receptor as a target for photochromic molecules.
AID343106Activity at GABAA alpha-2-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as potentiation of GABA-induced chloride current at 1 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343102Selectivity for GABAA alpha-5-beta-3-gamma-2 receptor over GABAA alpha-4-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID533781Binding affinity to human recombinant GABA alpha-4-beta-3-gamma-2 receptor2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
The GABA(A) receptor as a target for photochromic molecules.
AID1604586Binding affinity to GABA-A alpha2 (unknown origin) assessed as reduction in DMCM induced current relative to control
AID1604528Binding affinity to GABA-A alpha2 (unknown origin)
AID343402Binding affinity to GABAA alpha-1-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID71266Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-22000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
AID219795It is the ratio of Ki value for alpha-1-beta-3-gamma-2 to that of alpha-5-beta-3-gamma-21998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via compar
AID71699Binding affinity against Diazepam sensitive (DS) Gamma-aminobutyric acid A receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis of novel imidazobenzodiazepines as probes of the pharmacophore for "diazepam-insensitive" GABAA receptors.
AID219954Binding affinity against alpha-3-beta-3-gamma-2 GABAA/BzR receptor subtype.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via compar
AID73089Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-22000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
AID343110Inhibition of scopolamine-induced impairment of contextual memory in C57BL/6J mouse at 10 mg/kg, ip after 24 hrs2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID72132Binding affinity against Diazepam insensitive (DI) Gamma-aminobutyric acid A receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis of novel imidazobenzodiazepines as probes of the pharmacophore for "diazepam-insensitive" GABAA receptors.
AID1604590Selectivity ratio of Ki for binding affinity to GABAA alpha2beta3gamma2 (unknown origin) to Ki for binding affinity to GABAA alpha5beta3gamma2 (unknown origin)
AID343095Binding affinity to GABAA alpha-4-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343101Selectivity for GABAA alpha-5-beta-3-gamma-2 receptor over GABAA alpha-3-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343403Binding affinity to GABAA alpha-5-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID533779Binding affinity to human recombinant GABA alpha-2-beta-3-gamma-2 receptor2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
The GABA(A) receptor as a target for photochromic molecules.
AID1604589Selectivity ratio of Ki for binding affinity to GABAA alpha1beta3gamma2 (unknown origin) to Ki for binding affinity to GABAA alpha5beta3gamma2 (unknown origin)
AID1604588Binding affinity to GABA-A alpha5 (unknown origin) assessed as reduction in DMCM induced current relative to control
AID343104Activity at GABAA alpha-5-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as assessed as inhibition in GABA-induced current at 1 uM by voltage clamp assay2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID533778Binding affinity to human recombinant GABA alpha-1-beta-3-gamma-2 receptor2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
The GABA(A) receptor as a target for photochromic molecules.
AID1604530Binding affinity to GABA-A alpha3 (unknown origin)
AID73244Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-22000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
AID72927Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-22000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
AID1604587Binding affinity to GABA-A alpha3 (unknown origin) assessed as reduction in DMCM induced current relative to control
AID219940Binding affinity tested against alpha-2-beta-3-gamma-2 GABAA/BzR receptor subtype.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via compar
AID343099Selectivity for GABAA alpha-5-beta-3-gamma-2 receptor over GABAA alpha-1-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID1604531Binding affinity to GABA-A alpha5 (unknown origin)
AID1604529Binding affinity to GABA-A alpha1 (unknown origin)
AID343404Anticonvulsant activity in C57BL/6J mouse assessed as inhibition of increase in excitatory tone in brain at 30 mg/kg, ip2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343105Activity at GABAA alpha-1-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as potentiation of GABA-induced chloride current at 1 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID343100Selectivity for GABAA alpha-5-beta-3-gamma-2 receptor over GABAA alpha-2-beta-3-gamma-2 receptor2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
AID533780Binding affinity to human recombinant GABA alpha-3-beta-3-gamma-2 receptor2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
The GABA(A) receptor as a target for photochromic molecules.
AID73530Binding affinity for Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-21998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via compar
AID232720Selectivity ratio of alpha1 beta-3 gamma2 GABA A / BzR and alpha5 beta-3 gamma2 GABA A / BzR2000Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
AID343108Activity at GABAA alpha-6-beta-3-gamma-2 receptor expressed in Xenopus oocytes assessed as potentiation of GABA-induced chloride current at 1 uM2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (14.29)18.2507
2000's3 (21.43)29.6817
2010's7 (50.00)24.3611
2020's2 (14.29)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%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]