Page last updated: 2024-08-05 15:19:32

GABA-gated chloride channel antagonist

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ChEBI ID: 38999

Members (6)

MemberDefinitionClass
bicucullineA benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.bicuculline
chlordanchlordane
endosulfanA cyclic sulfite ester that is 1,5,5a,6,9,9a-hexahydro-6,9-methano-2,4,3-benzodioxathiepine 3-oxide substituted by chloro groups at positions 6, 7, 8, 9, 10 and 10.endosulfan
heptachlorA cyclodiene organochlorine insecticide that is 3a,4,7,7a-tetrahydro-1H-4,7-methanoindene substituted by chlorine atoms at positions 1, 4, 5, 6, 7, 8 and 8. Formerly used to kill termites, ants and other insects in agricultural and domestic situations.heptachlor
suraminA member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.suramin
suramin sodiumAn organic sodium salt that is the hexasodium salt of suramin. It is an FDA approved drug for African sleeping sickness and river blindness.suramin sodium

Research

Studies (11,303)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,899 (25.65)18.7374
1990's3,220 (28.49)18.2507
2000's3,014 (26.67)29.6817
2010's1,878 (16.62)24.3611
2020's292 (2.58)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials97 (0.81%)5.53%
Reviews297 (2.47%)6.00%
Case Studies129 (1.07%)4.05%
Observational1 (0.01%)0.25%
Other11,483 (95.64%)84.16%

Protein Targets (188)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
activating transcription factor 6Homo sapiens (human)Potency55.3991210
AR proteinHomo sapiens (human)Potency55.9906833
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency7.079511
Bloom syndrome protein isoform 1Homo sapiens (human)Potency1.258911
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency72.713414
caspase-1 isoform alpha precursorHomo sapiens (human)Potency39.810711
caspase-3Cricetulus griseus (Chinese hamster)Potency71.942415
caspase-3Homo sapiens (human)Potency72.713414
Caspase-7Cricetulus griseus (Chinese hamster)Potency71.942415
Cellular tumor antigen p53Homo sapiens (human)Potency68.3844211
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589311
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency23.587035
Chain A, Breast cancer type 1 susceptibility proteinHomo sapiens (human)Potency14.219112
Chain A, CruzipainTrypanosoma cruziPotency17.900812
Chain A, Ferritin light chainEquus caballus (horse)Potency28.183811
Chain A, HADH2 proteinHomo sapiens (human)Potency12.533123
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency22.106736
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency4.921326
Chain B, HADH2 proteinHomo sapiens (human)Potency12.533123
chromobox protein homolog 1Homo sapiens (human)Potency67.833412
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency11.052428
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency61.713716
DNA polymerase betaHomo sapiens (human)Potency0.891311
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.223911
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency50.706212
DNA polymerase kappa isoform 1Homo sapiens (human)Potency0.065812
endonuclease IVEscherichia coliPotency9.296122
estrogen nuclear receptor alphaHomo sapiens (human)Potency50.79831135
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency53.0539311
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency52.0817631
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency9.263413
EWS/FLI fusion proteinHomo sapiens (human)Potency10.476022
farnesoid X nuclear receptorHomo sapiens (human)Potency50.2786518
GABA theta subunitRattus norvegicus (Norway rat)Potency11.052414
galactokinaseHomo sapiens (human)Potency17.782811
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency11.052414
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency11.052414
gemininHomo sapiens (human)Potency2.310911
GLI family zinc finger 3Homo sapiens (human)Potency38.5052314
GLS proteinHomo sapiens (human)Potency8.912511
glucocerebrosidaseHomo sapiens (human)Potency22.387211
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency51.9627418
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency38.716222
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency8.912511
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency8.912511
heat shock protein beta-1Homo sapiens (human)Potency51.2178212
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency3.162312
Histone H2A.xCricetulus griseus (Chinese hamster)Potency95.9611212
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency11.034412
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency50.3473211
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency34.870533
importin subunit beta-1 isoform 1Homo sapiens (human)Potency70.794611
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency3.162311
Integrin alpha-IIbHomo sapiens (human)Potency12.589311
Integrin beta-3Homo sapiens (human)Potency12.589311
interleukin 8Homo sapiens (human)Potency45.196913
lamin isoform A-delta10Homo sapiens (human)Potency9.964823
lethal factor (plasmid)Bacillus anthracis str. A2012Potency22.474813
LuciferasePhotinus pyralis (common eastern firefly)Potency27.536222
M-phase phosphoprotein 8Homo sapiens (human)Potency8.912511
Microtubule-associated protein tauHomo sapiens (human)Potency23.182226
mitogen-activated protein kinase 1Homo sapiens (human)Potency1.000011
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency1.584911
NFKB1 protein, partialHomo sapiens (human)Potency0.354822
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency50.2048314
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency70.794611
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency55.6299211
Nuclear receptor ROR-gammaHomo sapiens (human)Potency19.819813
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency24.227627
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency31.622811
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.125411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency40.684047
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)Potency38.145612
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency49.3832410
phosphopantetheinyl transferaseBacillus subtilisPotency54.538812
Platelet-activating factor receptorHomo sapiens (human)Potency14.219112
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency3.162311
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency31.762613
pregnane X nuclear receptorHomo sapiens (human)Potency30.163127
pregnane X receptorRattus norvegicus (Norway rat)Potency44.668411
progesterone receptorHomo sapiens (human)Potency36.481829
pyruvate kinaseLeishmania mexicana mexicanaPotency0.794322
pyruvate kinase PKM isoform bHomo sapiens (human)Potency31.622822
RAR-related orphan receptor gammaMus musculus (house mouse)Potency51.8902211
regulator of G-protein signaling 4Homo sapiens (human)Potency0.007511
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency57.9946316
retinoid X nuclear receptor alphaHomo sapiens (human)Potency30.8995411
serine-protein kinase ATM isoform aHomo sapiens (human)Potency39.810711
SMAD family member 2Homo sapiens (human)Potency56.318325
SMAD family member 3Homo sapiens (human)Potency56.318325
snurportin-1Homo sapiens (human)Potency70.794611
survival motor neuron protein isoform dHomo sapiens (human)Potency11.220211
TDP1 proteinHomo sapiens (human)Potency15.309523
thioredoxin reductaseRattus norvegicus (Norway rat)Potency40.130412
ThrombopoietinHomo sapiens (human)Potency3.981122
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency41.4940313
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency50.118722
thyroid stimulating hormone receptorHomo sapiens (human)Potency15.8791518
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency40.850222
USP1 protein, partialHomo sapiens (human)Potency7.943311
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency33.6724212
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency55.363048
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency35.481311
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency68.519911

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
17-beta-hydroxysteroid dehydrogenase type 1Homo sapiens (human)IC5048.250011
Androgen receptorRattus norvegicus (Norway rat)IC5015.644013
ATP-dependent 6-phosphofructokinaseTrypanosoma brucei bruceiIC503.000011
Cathepsin BHomo sapiens (human)IC5030.000011
D(3) dopamine receptorRattus norvegicus (Norway rat)IC5018.100011
DNA primaseMycobacterium tuberculosis CDC1551IC508.200011
DNA-dependent protein kinase catalytic subunitHomo sapiens (human)IC501.700011
Dual specificity protein phosphatase 5Homo sapiens (human)Ki0.025011
Ectonucleoside triphosphate diphosphohydrolase 1Rattus norvegicus (Norway rat)Ki300.000022
Ectonucleoside triphosphate diphosphohydrolase 2Rattus norvegicus (Norway rat)Ki65.400022
Ectonucleoside triphosphate diphosphohydrolase 3 Rattus norvegicus (Norway rat)Ki12.700011
Ectonucleoside triphosphate diphosphohydrolase 8Homo sapiens (human)Ki100.000011
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC5015.000011
NAD-dependent protein deacetylase HST2Saccharomyces cerevisiae S288CIC50240.000011
NAD-dependent protein deacetylase sirtuin-1Homo sapiens (human)IC501.385777
NAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)IC501.175044
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC5020.600088
P2X purinoceptor 2Rattus norvegicus (Norway rat)IC5021.905412
P2Y purinoceptor 11Homo sapiens (human)Ki0.207122
P2Y purinoceptor 2Homo sapiens (human)IC5075.000022
P2Y purinoceptor 6Homo sapiens (human)IC5027.000011
Protein arginine N-methyltransferase 1Homo sapiens (human)IC50344.810033
Protein kinase C alpha typeHomo sapiens (human)IC5029.000011
Protein kinase C beta typeHomo sapiens (human)IC5029.000011
Protein kinase C delta typeHomo sapiens (human)IC5029.000011
Protein kinase C epsilon typeHomo sapiens (human)IC5029.000011
Protein kinase C eta typeHomo sapiens (human)IC5029.000011
Protein kinase C gamma typeHomo sapiens (human)IC5029.000011
Protein kinase C iota typeHomo sapiens (human)IC5029.000011
Protein kinase C theta typeHomo sapiens (human)IC5029.000011
Protein kinase C zeta typeHomo sapiens (human)IC5029.000011
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC5012.200022
RmtAAspergillus nidulansIC505.900011
Serine/threonine-protein kinase D1Homo sapiens (human)IC5029.000011
Serine/threonine-protein kinase D3Homo sapiens (human)IC5029.000011
Signal transducer and activator of transcription 1-alpha/betaHomo sapiens (human)IC509.100011
Signal transducer and activator of transcription 3 Mus musculus (house mouse)IC50100.000011
Signal transducer and activator of transcription 5AHomo sapiens (human)IC509.400011
Signal transducer and activator of transcription 5BHomo sapiens (human)IC5010.400011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC509.760011
Uracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)IC50100.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Delta-type opioid receptorHomo sapiens (human)EC50100.000011
Kappa-type opioid receptorHomo sapiens (human)EC50100.000011
Mu-type opioid receptorHomo sapiens (human)EC50100.000011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC501.300011
P2X purinoceptor 1Rattus norvegicus (Norway rat)EC501.000011
P2X purinoceptor 2Rattus norvegicus (Norway rat)EC5010.400011
P2X purinoceptor 3Homo sapiens (human)EC508.950022
P2X purinoceptor 4Rattus norvegicus (Norway rat)EC50100.000011
P2X purinoceptor 5Rattus norvegicus (Norway rat)EC504.000011
P2X purinoceptor 6Rattus norvegicus (Norway rat)EC50100.000011
P2X purinoceptor 7Homo sapiens (human)EC5092.000011
P2Y purinoceptor 1Meleagris gallopavo (turkey)EC5010.000011
P2Y purinoceptor 11Homo sapiens (human)EC5016.000011
P2Y purinoceptor 12Rattus norvegicus (Norway rat)EC504.000011
P2Y purinoceptor 2Homo sapiens (human)EC5048.000011
P2Y purinoceptor 4Homo sapiens (human)EC50100.000011