Page last updated: 2024-12-07

methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate

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

Description

methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID104999
CHEMBL ID17468
CHEMBL ID1256850
CHEBI ID92263
SCHEMBL ID472510
MeSH IDM0107071

Synonyms (50)

Synonym
9h-pyrido(3,4-b)indole-3-carboxylic acid, 4-ethyl-6,7-dimethoxy-, methyl ester
methyl 4-ethyl-6,7-dimethoxy-9h-pyrido(3,4-b)indole-3-carboxylate
4-ethyl-6,7-dimethoxy-9h-pyrido(3,4-b)indole-3-carboxylic acid, methyl ester
BRD-K14844937-001-01-6
PDSP2_001739
EU-0100543
lopac-e-007
NCGC00015392-01
PDSP1_001780
PDSP2_001763
BPBIO1_001013
LOPAC0_000543
PDSP1_001756
dmcm
BIOMOL-NT_000249
NCGC00093931-03
NCGC00093931-02
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate
NCGC00093931-01
NCGC00015392-02
E-007
CHEMBL17468 ,
82499-00-1
4-ethyl-6,7-dimethoxy-9h-carbazole-3-carboxylic acid methyl ester
4-ethyl-6,7-dimethoxy-9h-beta-carboline-3-carboxylic acid methyl ester
bdbm50065229
4-ethyl-6,7-dimethoxy-9h-beta-carboline-3-carboxylic acid methyl ester(dmcm)
methyl 4-ethyl-6,7-dimethoxy-9h-pyrido[3,4-b]indole-3-carboxylate
bdbm81951
cas_104999
nsc_104999
CHEMBL1256850
CCG-204633
NCGC00015392-03
NCGC00015392-04
unii-1309288n1j
1309288n1j ,
AKOS015897178
gtpl4179
methyl 6,7-dimethoxy-4-ethyl-.beta.-carboline-3-carboxylate
SCHEMBL472510
methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate
CHEBI:92263
AS-69508
sr-01000075869
SR-01000075869-1
DTXSID90896999
Q5205608
methyl 6,7-dimethoxy-4-ethyl-|a-carboline-3-carboxylate
methyl4-ethyl-6,7-dimethoxy-9h-pyrido[3,4-b]indole-3-carboxylate

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Complete dose-response curves were carried out on individual neurons, reducing error introduced by cell-to-cell variability."( Modulation of neurotransmitter action: control of the gamma-aminobutyric acid response through the benzodiazepine receptor.
Chan, CY; Farb, DH, 1985
)
0.27
" Midazolam (greater than 10(-6) M) reliably potentiated GABA responses with a parallel shift to the left of the dose-response curve."( Electrophysiological studies in cultured mouse CNS neurones of the actions of an agonist and an inverse agonist at the benzodiazepine receptor.
Jensen, MS; Lambert, JD, 1986
)
0.27
" Dose-response and time course studies of Ro 15-4513 against gamma-aminobutyric acid (GABA) antagonists were performed."( Interactions of the imidazodiazepine Ro 15-4513 with chemical convulsants.
Lister, RG; Nutt, DJ, 1988
)
0.27
" Midazolam (10(-7)-10(-5) M) potentiated responses to all three agonists to a similar extent with a shift to the left of the dose-response curve."( Modulation of the responses to the GABA-mimetics, THIP and piperidine-4-sulphonic acid, by agents which interact with benzodiazepine receptors. An electrophysiological study on cultured mouse neurones.
Jensen, MS; Lambert, JD, 1984
)
0.27
" The dose-response relationship of DMCM and changes in antibody levels was nonmonotonic, with high doses resulting in an increase in serum antibody levels and moderate doses resulting in a decrease in serum antibody levels."( Modulation of the in vivo antibody response by a benzodiazepine inverse agonist (DMCM) administered centrally or peripherally.
Brohm, MM; Fleshner, M; Laudenslager, ML; Maier, SF; Watkins, LR, 1993
)
0.29
" Dose-response relationships for GABA were compared in the absence and presence of 1 microM diazepam (DZP) or methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM)."( Mechanism of action of benzodiazepines on GABAA receptors.
Campo-Soria, C; Chang, Y; Weiss, DS, 2006
)
0.33
" The goal of the present study was to examine the influence of the inverse agonist methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM) acting on α GABA(A) receptor and compare its dose-response effects on memory and depression-like behavior."( DMCM, a benzodiazepine site inverse agonist, improves active avoidance and motivation in the rat.
Obradović, DI; Obradović, M; Oprić, D; Samardžić, J; Strac, DŠ, 2012
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
beta-carbolinesAny pyridoindole containing a beta-carboline skeleton and their hydrogenated derivatives
[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 (51)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency6.30960.003245.467312,589.2998AID1705
Chain A, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.62280.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID2323
endonuclease IVEscherichia coliPotency10.00000.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency44.66840.100020.879379.4328AID588453
NFKB1 protein, partialHomo sapiens (human)Potency5.62340.02827.055915.8489AID895; AID928
TDP1 proteinHomo sapiens (human)Potency7.35630.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency2.66510.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency10.00000.00137.762544.6684AID914; AID915
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.30960.001318.074339.8107AID926
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency35.48130.28189.721235.4813AID2326
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02240.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency8.91250.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency37.933023.934123.934123.9341AID1967
DNA polymerase betaHomo sapiens (human)Potency35.48130.022421.010289.1251AID485314
mitogen-activated protein kinase 1Homo sapiens (human)Potency7.94330.039816.784239.8107AID995
DNA polymerase eta isoform 1Homo sapiens (human)Potency22.38720.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency22.38720.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency15.84890.004611.374133.4983AID463097
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.84890.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency0.79430.177824.735279.4328AID488949
caspase-1 isoform alpha precursorHomo sapiens (human)Potency19.95260.000311.448431.6228AID900
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency9.50560.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.00400.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.84891.000012.224831.6228AID885
[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)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.00910.00000.21085.6234AID219791; AID239699; AID72918; AID72919; AID72927; AID72930; AID72934; AID73066
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.01460.00000.18819.0000AID219791; AID219938; AID219953; AID239699; AID239700; AID239701; AID239702; AID71266; AID71267; AID72918; AID72919; AID72927; AID72930; AID72934; AID73066; AID73080; AID73081; AID73089; AID73090; AID73094; AID73217; AID73235; AID73236; AID73244; AID73245; AID73246; AID73361; AID73381; AID73382; AID73523; AID73526; AID73529; AID73531; AID73532
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.00760.00020.561410.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.00760.00020.635210.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.00760.00020.621710.0000AID40670
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.00760.00020.675810.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.00760.00020.646910.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.01460.00010.20769.0000AID219791; AID219938; AID219953; AID239699; AID239700; AID239701; AID239702; AID71266; AID71267; AID72918; AID72919; AID72927; AID72930; AID72934; AID73066; AID73080; AID73081; AID73089; AID73090; AID73094; AID73217; AID73235; AID73236; AID73244; AID73245; AID73246; AID73361; AID73381; AID73382; AID73523; AID73526; AID73529; AID73531; AID73532
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.00760.00020.671210.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.00180.00010.24425.6234AID239702; AID73381; AID73382; AID73523; AID73526; AID73529; AID73531; AID73532
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.00650.00010.25155.6234AID219953; AID239701; AID73235; AID73236; AID73244; AID73245; AID73246; AID73361
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki0.01100.00010.24015.6234AID219938; AID239700; AID73080; AID73081; AID73089; AID73090; AID73094; AID73217
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.00760.00020.557710.0000AID40670
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.00760.00020.640310.0000AID40670
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.00760.00020.570810.0000AID40670
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.13400.00020.41199.0000AID71266; AID71267
GABA theta subunitRattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.00760.00020.656110.0000AID40670
[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)
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)EC50 (µMol)0.00900.00112.000910.0000AID548175
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)EC50 (µMol)0.00900.00141.957810.0000AID548175; AID548176; AID548177; AID548178
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)EC50 (µMol)0.00900.00301.65329.8000AID548176; AID548177; AID548178
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)EC50 (µMol)0.00300.00301.58219.8000AID548178
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)EC50 (µMol)0.01000.01001.20095.6234AID548177
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)EC50 (µMol)0.01400.01201.17515.2000AID548176
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)EC50 (µMol)0.00900.00141.776810.0000AID548175
[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 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)
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)
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)
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 (23)

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 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)
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 (80)

Assay IDTitleYearJournalArticle
AID72922Modulatory effect on coapplication with GABA at human Gamma-aminobutyric acid A receptor alpha-1-beta-3-gamma-2 in Xenopus oocyte.2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
AID73236Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-3-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID72910Percentage modulation of submaximal (EC20) response to GABA in Xenopus oocytes expressing human GABA-A alpha-1-beta-3-gamma-2 subunits2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID548169Negative allosteric modulation of human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes at 1 uM2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID73241Efficacy for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-)cells2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID73526Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-5-beta-3-gamma-2) stably expressed in L(tk-) cells.2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID73080Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-22004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID548167Negative allosteric modulation of human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes at 1 uM2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID72930Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-1-beta-3-gamma-2) stably expressed in L(tk-) cells.2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
AID71267Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-21998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423)
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID73520Efficacy for GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in Xenopus laevis oocytes by two-electrode voltage clamp recording2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID73531Binding affinity to human GABA A alpha-5-beta-3-gamma-2 receptor, using a [3H]-Ro- 15-1788 radioligand2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID73073Percentage modulation of submaximal (EC20) response to GABA in Xenopus oocytes expressing human GABA-A alpha-2-beta-3-gamma-2 subunits2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID73532Displacement of [3H]- Ro 15-1788 binding from human GABA-A receptor alpha-5-beta-3-gamma-2 subunits2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID243405In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID72918Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-22004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID239701Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells 2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID73388Selectivity for GABA-A receptor alpha-5 subunit over alpha1,2,3 (range 3-6)2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID548175Binding affinity to human alpha1beta2gamma2 GABA receptor expressed in Xenopus laevis oocytes2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID73086Efficacy for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-)cells2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID219791Binding affinity measured using LtK- cell membranes expressing GABA alpha-1-beta-3-gamma-2 receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423)
AID73069Maximum modulation relative to GABA EC20 against human GABA-A receptor alpha-1-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-) cells2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID72934Binding affinity to human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2, determined using [3H]-Ro- 15-1788 radioligand2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID73219Maximum modulation relative to GABA EC20 against human GABA-A receptor alpha-2-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-) cells2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID239702Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells 2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID73245Binding affinity by displacement of [3H]Ro-151788 from recombinant human gamma-aminobutyric-acid A receptor alpha3,beta3,gamma2 stably expressed in L cells2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
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.
AID243407In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID219938Binding affinity measured using LtK- cell membranes expressing GABA alpha-2-beta-3-gamma-2 receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423)
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.
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.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID548176Binding affinity to human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID73094Binding affinity to human gamma-amino butyric-acid A receptor alpha-2-beta-3-gamma-2, using a [3H]-Ro- 15-1788 radioligand2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID243406In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID73374Percentage modulation of submaximal (EC20) response to GABA in Xenopus oocytes expressing human GABA-A alpha-5-beta-3-gamma-2 subunits2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID239700Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells 2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID73370Percentage modulation of GABA EC20 against human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in Xenopus laevis oocytes2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID73090Displacement of [3H]Ro-151788 from human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 stably expressed in L(tk-) cells2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
AID243404In vitro percent efficacy against human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID73372Percentage modulation of submaximal (EC20) response to GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in Xenopus laevis oocytes2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID239699Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells 2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
AID219953Binding affinity measured using LtK- cell membranes expressing GABA alpha-3-beta-3-gamma-2 receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423)
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID73373Percentage modulation of submaximal (EC20) response to GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in mouse fibroblast L(tk-) cells2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID73227Percentage modulation of submaximal (EC20) response to GABA in Xenopus oocytes expressing human GABA-A alpha-3-beta-3-gamma-2 subunits2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID73361Displacement of [3H]- Ro 15-1788 binding from human GABA-A receptor alpha-3-beta-3-gamma-2 subunits2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID73518Efficacy for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-)cells2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID72924Efficacy for human GABA-A receptor alpha-1-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-)cells2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID73363Maximum modulation relative to GABA EC20 against human GABA-A receptor alpha-3-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-) cells2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID73237Modulatory effect on coapplication with GABA at human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 in Xenopus oocytes.2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
AID548166Negative allosteric modulation of human alpha1beta2gamma2 GABA receptor expressed in Xenopus laevis oocytes at 1 uM2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID73381Inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-5-beta-3-gamma-2 subunits2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID72636Selectivity for GABA-A receptor alpha-5 subunit binding over alpha-1,2,3 when co-expressed with beta-3 and gamma-22002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID73246Binding affinity to human gamma-amino butyric-acid A receptor alpha-3-beta-3-gamma-2, using a [3H]-Ro- 15-1788 radioligand2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID40670In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand).1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Structure-activity relationships and molecular modeling analysis of flavonoids binding to the benzodiazepine site of the rat brain GABA(A) receptor complex.
AID226428Ratio of Ki value without GABA and Ki value in the presence of GABA.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Structure-activity relationships and molecular modeling analysis of flavonoids binding to the benzodiazepine site of the rat brain GABA(A) receptor complex.
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.
AID73536Maximum modulation relative to GABA EC20 against human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in mammalian fibroblast L(tk-) cells2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID73217Displacement of [3H]- Ro 15-1788 binding from human GABA-A receptor alpha-2-beta-3-gamma-2 subunits2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID73235Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-22004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
AID72919Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-1-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID548178Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID548177Binding affinity to human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID73529Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-21998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423)
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.
AID548168Negative allosteric modulation of human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes at 1 uM2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Developing dual functional allosteric modulators of GABA(A) receptors.
AID72637Binding selectivity for human gamma-aminobutyric-acid A receptor alpha-5 over GABA A alpha1,alpha2 and alpha-3 receptors2003Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
AID73066Displacement of [3H]- Ro 15-1788 binding from human GABA-A receptor alpha-1-beta-3-gamma-2 subunits2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID73382Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-5-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID73081Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-2-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
AID73083Modulatory effect on coapplication with GABA at human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed inXenopus oocytes2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (214)

TimeframeStudies, This Drug (%)All Drugs %
pre-199083 (38.79)18.7374
1990's72 (33.64)18.2507
2000's39 (18.22)29.6817
2010's17 (7.94)24.3611
2020's3 (1.40)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.89

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 Index8.89 (24.57)
Research Supply Index5.39 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews7 (3.21%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other211 (96.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]