Page last updated: 2024-11-07

cl 218872

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Description

CL 218872: shows specific action on benzodiazepine receptors; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID107950
CHEMBL ID13662
CHEBI ID92018
SCHEMBL ID1320758
MeSH IDM0076783

Synonyms (55)

Synonym
unii-o7gr5xl5b5
o7gr5xl5b5 ,
cl-218,872
HMS3268A16
BRD-K00662280-001-01-1
cl-218872
PDSP1_000634
NCGC00025269-01
tocris-1709
PDSP2_000629
PDSP1_001766
PDSP2_001749
smr000326924
MLS000860066
1,2,4-triazolo(4,3-b)pyridazine, 3-methyl-6-(3-(trifluoromethyl)phenyl)-
cl 218872
3-methyl-6-(3-(trifluoromethyl)phenyl)-1,2,4-triazolo(4,2-b)pyridazine
66548-69-4
cl218,872
ci-218872
CHEMBL13662 ,
3-methyl-6-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[4,3-b]pyridazine
bdbm50026756
v3-methyl-6-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[4,3-b]pyridazine
3-methyl-6-[3-(trifluoromethyl)phenyl]-[1,2,4]triazolo[4,3-b]pyridazine
A835489
NCGC00025269-02
SCHEMBL1320758
HMS2235F15
FT-0641074
HMS3369C09
3-methyl-6-(alpha,alpha,alpha-trifluoro-m-tolyl)-1,2,4-triazolo[4,3-b]pyridazine
3-methyl-6-(alpha, alpha,alpha -trifluoro-m-tolyl)-1,2,4-triazolo[4,3-b]pyridazine
AKOS024456755
3-methyl-6-[-3-(trifluoromethyl)phenyl]-1,2,4-triazolo[4,3-b]pyridazine
AC-33570
Z2026966425
DTXSID80216728
J-520102
1,2,4-triazolo[4,3-b]pyridazine, 3-methyl-6-[3-(trifluoromethyl)phenyl]-
sr-01000597518
SR-01000597518-1
3-methyl-6-(3-[trifluoromethyl]phenyl)-1,2,4-triazolo-(4,3-b)pyridazine
CHEBI:92018
Q5012653
HMS3676D18
HMS3412D18
BRD-K00662280-001-04-5
3-methyl-6-[3-(trifluoromethyl)phenyl]-1,2,4-triazolo-(4,3-b)pyridazine
3-methyl-6-(3-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-b]pyridazine
cl218872
3-methyl-6(3-(trifluoromethyl)phenyl)-1,2,4-triazolo (4.3-b)pyridazine
CS-0028007
HY-103505
EN300-208442

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of several compounds believed to act at the GABA-benzodiazepine receptor complex and which have anticonvulsant or proconvulsant properties when administered in combination with picrotoxin and pentetrazol (leptazol, pentylenetetrazole) were investigated in combination with the convulsant benzodiazepine Ro 5-4864."( Pro- and anti-convulsant drug effects in combination with the convulsant benzodiazepine Ro 5-4864.
File, SE; Pellow, S, 1985
)
0.27

Bioavailability

ExcerptReferenceRelevance
" Compound 62 is currently one of the most binding selective GABA-A alpha 3-benzodiazepine-site partial agonists known, and although its selectivity is limited, its good pharmacokinetic profile in the rat (33% oral bioavailability after a 3 mg/kg dose, reaching a peak plasma concentration of 179 ng/mL; half-life of 1 h) made it a useful pharmacological tool to explore the effect of a GABA-A alpha 2/alpha 3 agonist in vivo."( 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Atack, JR; Carling, RW; Castro, JL; Cook, SM; Dawson, GR; Ferris, P; Isted, C; Leeson, PD; McKernan, RM; Moore, KW; O'Connor, D; Quirk, K; Street, LJ; Thomas, S; Thompson, SA; Wafford, KA; Wild, D, 2004
)
0.32

Dosage Studied

ExcerptRelevanceReference
" Comparison of the dose-response curves demonstrated a difference in the intensity of the stimulus effects."( The discriminative stimulus effects of diazepam in rats at two training doses.
Franklin, SR; Tang, AH, 1991
)
0.28
" 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
" Diazepam shifted GABA dose-response curves to the left by decreasing the apparent KD but without altering the apparent Vmax (Lineweaver-Burk analysis)."( Benzodiazepine receptor ligand actions on GABA responses. Benzodiazepines, CL 218872, zopiclone.
Macdonald, RL; Skerritt, JH, 1984
)
0.5
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
pyridazines
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
[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 (36)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.79430.004023.8416100.0000AID485290
Chain A, HADH2 proteinHomo sapiens (human)Potency19.95260.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency19.95260.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.62280.177814.390939.8107AID2147
thioredoxin reductaseRattus norvegicus (Norway rat)Potency89.12510.100020.879379.4328AID588456
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency0.16830.531815.435837.6858AID504845
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency31.62280.001815.663839.8107AID894
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
gemininHomo sapiens (human)Potency28.18380.004611.374133.4983AID624297
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency31.62280.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency100.00003.981146.7448112.2020AID720708
GABA theta subunitRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
[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)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.05880.00000.21085.6234AID219791; AID239564; AID527597; AID72467; AID72927
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki2.04940.00000.18819.0000AID219791; AID219938; AID219953; AID239563; AID239564; AID239565; AID239566; AID527597; AID527598; AID527599; AID527601; AID527602; AID71266; AID71267; AID72467; AID72477; AID72620; AID72625; AID72927; AID73089; AID73244; AID73523; AID73529
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.505710.0000AID40661
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki3.73620.00020.561410.0000AID219782; AID219783; AID219947; AID220441; AID220443; AID220445; AID220446; AID220448; AID40970
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.497310.0000AID40661
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.19800.00020.635210.0000AID40970
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.90900.00020.621710.0000AID219947; AID40970
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.498810.0000AID40661
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.19800.00020.675810.0000AID40970
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.504610.0000AID40661
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.19800.00020.646910.0000AID40970
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki2.04940.00010.20769.0000AID219791; AID219938; AID219953; AID239563; AID239564; AID239565; AID239566; AID527597; AID527598; AID527599; AID527601; AID527602; AID71266; AID71267; AID72467; AID72477; AID72620; AID72625; AID72927; AID73089; AID73244; AID73523; AID73529
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki3.64970.00020.671210.0000AID220441; AID220443; AID220445; AID220446; AID220448; AID40970
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)Ki0.54060.00010.24425.6234AID239566; AID527601; AID72625; AID73523; AID73529
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki1.10640.00010.25155.6234AID219953; AID239565; AID527599; AID72620; AID73244
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)Ki1.72160.00010.24015.6234AID219938; AID239563; AID527598; AID72477; AID73089
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.506510.0000AID40661
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki3.43530.00020.557710.0000AID219782; AID219783; AID40970
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.505710.0000AID40661
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.19800.00020.640310.0000AID40970
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki3.73620.00020.570810.0000AID219782; AID219783; AID219947; AID220441; AID220443; AID220445; AID220446; AID220448; AID40970
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki10.00000.00000.73078.0000AID220441
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki10.00000.00020.41199.0000AID527602; AID71266; AID71267
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
GABA theta subunitRattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.11600.00010.507510.0000AID40661
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.19800.00020.656110.0000AID40970
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

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)
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)
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

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-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)
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

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-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)
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID177658Effect on phenylenetetrazole seizures at 5 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID219782Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID239564Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
AID177653Effect on phenylenetetrazole seizures at 0.5 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID40663In vitro inhibition of [3H]diazepam binding towards Benzodiazepine receptor at 1 uM1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID220128Binding affinity for rat GABA-A receptor alpha-4-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
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.
AID220441Binding affinity for rat GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
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.
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)
AID177656Effect on phenylenetetrazole seizures at 3 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID72467Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
AID40661In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID239565Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 subtype expressed in L (tk-) cells2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 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.
AID220446Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID220445Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID129147Anticonvulsant activity of the compound when maximal electroshock is induced in mouse1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands.
AID219783Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID239566Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 subtype expressed in L (tk-) cells2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
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.
AID128166Activity was measured by rotarod test by intraperitoneal administration in mouse.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands.
AID177063Anxiolytic activity for protection against pentylenetetrazole-induced convulsions in experiment 11981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID129146Anticonvulsant activity of the compound when lethal dose of strychnine given subcutaneously in mouse1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands.
AID72620Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
AID40970In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties.
AID527602Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-6-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
AID220130Binding affinity for mutant rat GABA-A receptor alpha-4-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
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.
AID72138Binding affinity to rat chimeric GABA-A receptor C6, alpha1-alpha6 chimeric subunit co-expressed with beta-2 gamma2 subunits in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID177657Effect on phenylenetetrazole seizures at 4 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID527599Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
AID177659Effect on phenylenetetrazole seizures at 6 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID72477Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
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)
AID177654Effect on phenylenetetrazole seizures at 1 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID219947Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID177655Effect on phenylenetetrazole seizures at 2 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID72625Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
AID220448Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID177064Anxiolytic activity for protection against pentylenetetrazole-induced convulsions in experiment 21981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID239563Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells2005Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
AID220443Binding affinity for mutant rat GABA-A receptor alpha-6-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
AID527597Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
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)
AID226274Relative binding to GABA-A central benzodiazepine receptor in the presence and absence of 10e-4 M GABA (GABA shift)1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant 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)
AID177660Effect on phenylenetetrazole seizures at 7 hr in rat1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines.
AID220296Binding affinity for rat GABA-A receptor alpha-5--beta-2-gamma-2 subunits expressed in HEK293 cells1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
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)
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.
AID527598Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
AID527601Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-5-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (154)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990101 (65.58)18.7374
1990's36 (23.38)18.2507
2000's10 (6.49)29.6817
2010's4 (2.60)24.3611
2020's3 (1.95)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.56

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index31.56 (24.57)
Research Supply Index5.07 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index44.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews8 (5.06%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other150 (94.94%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]