Page last updated: 2024-08-07 15:59:40

Gamma-aminobutyric acid receptor subunit alpha-1

A gamma-aminobutyric acid receptor subunit alpha-1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14867]

Synonyms

GABA(A) receptor subunit alpha-1

Research

Bioassay Publications (96)

TimeframeStudies on this Protein(%)All Drugs %
pre-19903 (3.13)18.7374
1990's12 (12.50)18.2507
2000's42 (43.75)29.6817
2010's32 (33.33)24.3611
2020's7 (7.29)2.80

Compounds (140)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
gamma-aminobutyric acidHomo sapiens (human)Ki0.116522
phenytoinHomo sapiens (human)Ki100.000011
alprazolamHomo sapiens (human)Ki0.000811
chlordiazepoxideHomo sapiens (human)Ki0.635044
clonazepamHomo sapiens (human)IC50555,904.000011
clonazepamHomo sapiens (human)Ki0.000811
nordazepamHomo sapiens (human)IC50106,414.000011
diazepamHomo sapiens (human)IC5041,198.340033
diazepamHomo sapiens (human)Ki0.01301414
fipronilHomo sapiens (human)IC500.002311
flumazenilHomo sapiens (human)Ki0.0049732
flunitrazepamHomo sapiens (human)IC50263,027.000011
flunitrazepamHomo sapiens (human)Ki0.002644
fluoxetineHomo sapiens (human)IC505.200012
hydroxyureaHomo sapiens (human)Ki113.000012
isoguvacineHomo sapiens (human)Ki0.055012
4-piperidinecarboxylic acidHomo sapiens (human)Ki0.505612
kynurenic acidHomo sapiens (human)IC502,900.000011
muscimolHomo sapiens (human)IC500.016011
muscimolHomo sapiens (human)Ki0.008522
nitrazepamHomo sapiens (human)IC50100,000.000011
cm 7116Homo sapiens (human)IC50500,035.000011
pentobarbitalHomo sapiens (human)IC501,000.000011
propofolHomo sapiens (human)IC5028.000033
ro 15-4513Homo sapiens (human)Ki0.009467
temazepamHomo sapiens (human)IC5062,517.300011
triazolamHomo sapiens (human)Ki0.000811
zolpidemHomo sapiens (human)Ki1.39591138
triiodothyronineHomo sapiens (human)IC5023.000011
bicucullineHomo sapiens (human)IC5015.000011
flavoneHomo sapiens (human)Ki0.508522
chlordesmethyldiazepamHomo sapiens (human)IC50277,952.001422
6-aminonicotinic acidHomo sapiens (human)Ki4.236912
halazepamHomo sapiens (human)IC5010,864.300011
phenazepamHomo sapiens (human)Ki0.000011
progabideHomo sapiens (human)Ki40.000011
duloxetineHomo sapiens (human)IC500.019012
norharmanHomo sapiens (human)IC501.621811
baicalinHomo sapiens (human)Ki77.624711
abecarnilHomo sapiens (human)Ki0.012422
2-aminonicotinic acidHomo sapiens (human)Ki100.000011
n-desmethylflunitrazepamHomo sapiens (human)IC5025,003.500011
7-aminonitrazepamHomo sapiens (human)IC502,588.210011
ro 20-1815Homo sapiens (human)IC5015,381.500011
brexanoloneHomo sapiens (human)IC500.022011
2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-oneHomo sapiens (human)IC500.000111
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylateHomo sapiens (human)Ki0.009188
beta-carboline-3-carboxylic acid ethyl esterHomo sapiens (human)IC500.005011
beta-carboline-3-carboxylic acid ethyl esterHomo sapiens (human)Ki0.001233
beta-carboline-3-carboxylic acid methyl esterHomo sapiens (human)IC500.005011
sr 95531Homo sapiens (human)IC500.276333
sr 95531Homo sapiens (human)Ki0.240011
bretazenilHomo sapiens (human)Ki0.000411
cl 218872Homo sapiens (human)Ki0.058855
ro 15-3505Homo sapiens (human)Ki0.006844
zk 93426Homo sapiens (human)Ki0.137011
zk 93423Homo sapiens (human)Ki0.004122
3-ethoxy-beta-carbolineHomo sapiens (human)IC500.024011
3-ethoxy-beta-carbolineHomo sapiens (human)Ki0.006433
tert-butyl beta-carboline-3-carboxylateHomo sapiens (human)IC500.010011
tert-butyl beta-carboline-3-carboxylateHomo sapiens (human)Ki0.000733
5-(4-piperidyl)isoxazol-3-olHomo sapiens (human)IC50500.593512
5-(4-piperidyl)isoxazol-3-olHomo sapiens (human)Ki11.000011
ro 14-7437Homo sapiens (human)Ki0.001211
3',6-dinitroflavoneHomo sapiens (human)Ki0.012011
l 663581Homo sapiens (human)Ki0.000411
cgp 36742Homo sapiens (human)IC50508.000022
pitrazepinHomo sapiens (human)IC500.240011
7-aminoclonazepamHomo sapiens (human)IC5013,335.200011
zg 63Homo sapiens (human)Ki0.017322
ro 5-3438Homo sapiens (human)IC5071,449.600011
cocaineHomo sapiens (human)IC50127.000011
6-bromoflavoneHomo sapiens (human)Ki0.070811
n-desmethylflunitrazepamHomo sapiens (human)IC50666,807.000011
ro 05-4082Homo sapiens (human)IC50454,988.000011
l 364373Homo sapiens (human)IC50100.000011
etomidateHomo sapiens (human)IC50577.000011
eszopicloneHomo sapiens (human)Ki0.050111
1-(1h-indol-3-ylcarbonyl)-n-(4-methoxybenzyl)formamideHomo sapiens (human)Ki0.162211
2-[(2-ethoxyphenoxy)-phenylmethyl]morpholineHomo sapiens (human)IC500.011012
panadiplonHomo sapiens (human)Ki0.003511
meclonazepamHomo sapiens (human)IC50833,681.000011
isothazHomo sapiens (human)IC5016.000011
n-(indol-3-ylglyoxylyl)benzylamineHomo sapiens (human)Ki0.120211
6-bromo-3'-nitroflavoneHomo sapiens (human)Ki0.001011
3-propoxy-beta-carbolineHomo sapiens (human)IC500.011011
3-propoxy-beta-carbolineHomo sapiens (human)Ki0.005333
apigeninHomo sapiens (human)Ki3.020011
harmanHomo sapiens (human)IC5012.302711
amentoflavoneHomo sapiens (human)IC50281,838.000011
amentoflavoneHomo sapiens (human)Ki0.006022
baicaleinHomo sapiens (human)Ki5.623411
chrysinHomo sapiens (human)Ki3.020011
hispidulinHomo sapiens (human)Ki1.000011
scutellareinHomo sapiens (human)Ki12.022611
wogoninHomo sapiens (human)Ki2.041711
cholesta-3,5-dien-7-oneHomo sapiens (human)IC5011.250022
l 655,708Homo sapiens (human)Ki0.043477
ry 80Homo sapiens (human)Ki0.0234712
1-Ethyl-9H-pyrido[3,4-b]indoleHomo sapiens (human)IC50251.189011
3-[(1S)-1-phenylethyl]-4-imidazolecarboxylic acid ethyl esterHomo sapiens (human)IC50295.000011
ganaxoloneHomo sapiens (human)IC500.042011
mrk 016Homo sapiens (human)Ki0.000833
6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5h)-oneHomo sapiens (human)Ki0.020022
bis(7)-tacrineHomo sapiens (human)IC506.000011
2-pyridin-2-yl-4h-1,3-benzothiazin-4-oneHomo sapiens (human)Ki0.934010
qh-ii-66Homo sapiens (human)Ki0.076322
l 838,417Homo sapiens (human)Ki0.000822
ry 024Homo sapiens (human)Ki0.026955
pwz-029Homo sapiens (human)Ki0.436455
naluzotanHomo sapiens (human)Ki2.000011
basimglurantHomo sapiens (human)Ki3.160011
ro 4956371Homo sapiens (human)Ki3.160011
mln8054Homo sapiens (human)IC500.330011
mdv 3100Homo sapiens (human)IC503.000011
ns 11394Homo sapiens (human)Ki0.000411
valproate sodiumHomo sapiens (human)Ki100.000011
mrk-409Homo sapiens (human)Ki0.000211
4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propylcinnoline-3-carboxamideHomo sapiens (human)Ki0.000511
4-amino-8-(2,5-dimethoxyphenyl)-n-propylcinnoline-3-carboxamideHomo sapiens (human)Ki0.000511
pf 04457845Homo sapiens (human)Ki1.140110
mln 8237Homo sapiens (human)IC500.490011
apalutamideHomo sapiens (human)IC503.000011
nitd 609Homo sapiens (human)IC5010.000011
mk-7246Homo sapiens (human)Ki1.115010
a-1155463Homo sapiens (human)Ki0.794010

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
gamma-aminobutyric acidHomo sapiens (human)EC5020.7620913
benzyl alcoholHomo sapiens (human)EC5050,000.000011
phenolHomo sapiens (human)EC5050,500.000022
alprazolamHomo sapiens (human)EC500.037011
diazepamHomo sapiens (human)EC500.092522
diazepamHomo sapiens (human)Kd0.036011
flumazenilHomo sapiens (human)Kd0.002011
flunitrazepamHomo sapiens (human)EC500.001411
flunitrazepamHomo sapiens (human)Kd0.004511
gaboxadolHomo sapiens (human)EC5014.062712
isoguvacineHomo sapiens (human)EC5060.740123
4-piperidinecarboxylic acidHomo sapiens (human)EC50620.000011
muscimolHomo sapiens (human)EC505.830835
piperidine-4-sulfonic acidHomo sapiens (human)EC5040.000011
propofolHomo sapiens (human)EC5019.855099
ro 15-4513Homo sapiens (human)EC500.001111
ro 15-4513Homo sapiens (human)Kd0.003311
triazolamHomo sapiens (human)Kd0.001011
zaleplonHomo sapiens (human)EC500.290011
zolpidemHomo sapiens (human)EC500.209733
2-isopropylphenolHomo sapiens (human)EC5099.149822
pyrogallol 1,3-dimethyl etherHomo sapiens (human)EC50100,000.000022
2,4-di-tert-butylphenolHomo sapiens (human)EC50100,000.000022
ostholHomo sapiens (human)EC5014.000011
2,6-xylenolHomo sapiens (human)EC50162.709522
2,6-dibromophenolHomo sapiens (human)EC50100,000.000022
6-aminonicotinic acidHomo sapiens (human)EC50308.114012
2,6-di-tert-butylphenolHomo sapiens (human)EC50100,000.000022
oxypeucadanin, (s)-(-)-isomerHomo sapiens (human)EC5025.000011
abecarnilHomo sapiens (human)Kd0.001011
magnololHomo sapiens (human)EC5020.800022
honokiolHomo sapiens (human)EC5058.025044
brexanoloneHomo sapiens (human)EC500.177444
imidazoleacetic acidHomo sapiens (human)EC50126.917035
2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-oneHomo sapiens (human)Kd0.000111
alphaxaloneHomo sapiens (human)EC501.050033
methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylateHomo sapiens (human)EC500.009011
beta-carboline-3-carboxylic acid ethyl esterHomo sapiens (human)Kd0.001011
beta-carboline-3-carboxylic acid methyl esterHomo sapiens (human)Kd0.001011
3-ethoxy-beta-carbolineHomo sapiens (human)Kd0.001211
tert-butyl beta-carboline-3-carboxylateHomo sapiens (human)Kd0.001011
4-methoxyhonokiolHomo sapiens (human)EC5027.200011
piperineHomo sapiens (human)EC5029.100022
etomidateHomo sapiens (human)EC5019.675044
loreclezoleHomo sapiens (human)EC5011.000011
3-propoxy-beta-carbolineHomo sapiens (human)Kd0.005011
amentoflavoneHomo sapiens (human)EC503.600011
stiripentolHomo sapiens (human)EC5046.000011
3-[(1S)-1-phenylethyl]-4-imidazolecarboxylic acid ethyl esterHomo sapiens (human)EC5047.000011
valerenic acidHomo sapiens (human)EC5015.800022
ganaxoloneHomo sapiens (human)EC500.209733
qh-ii-66Homo sapiens (human)Kd0.076011
4-iodo-2,6-diisopropylphenolHomo sapiens (human)EC5026.155744
ry 024Homo sapiens (human)EC5074.400011
batatasin-iiiHomo sapiens (human)EC5067.200011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
(1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acidHomo sapiens (human)Kb320.000022
3-[(1S)-1-phenylethyl]-4-imidazolecarboxylic acid ethyl esterHomo sapiens (human)Concentration100.000011

Enables

This protein enables 3 target(s):

TargetCategoryDefinition
GABA-A receptor activitymolecular functionCombining with the amino acid gamma-aminobutyric acid (GABA, 4-aminobutyrate) to initiate a change in cell activity. GABA-A receptors function as chloride channels. [PMID:8974333]
GABA-gated chloride ion channel activitymolecular functionEnables the transmembrane transfer of a chloride ion by a channel that opens when GABA has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport, ISBN:0815340729]
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialmolecular functionAny transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227]

Located In

This protein is located in 4 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
cytoplasmic vesicle membranecellular componentThe lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah]
GABA-ergic synapsecellular componentA synapse that uses GABA as a neurotransmitter. These synapses are typically inhibitory. [GOC:dos]
postsynaptic specialization membranecellular componentThe membrane component of the postsynaptic specialization. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos]

Active In

This protein is active in 5 target(s):

TargetCategoryDefinition
dendrite membranecellular componentThe portion of the plasma membrane surrounding a dendrite. [GOC:mah]
postsynapsecellular componentThe part of a synapse that is part of the post-synaptic cell. [GOC:dos]
synapsecellular componentThe junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]
neuron projectioncellular componentA prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Part Of

This protein is part of 4 target(s):

TargetCategoryDefinition
GABA-A receptor complexcellular componentA protein complex which is capable of GABA-A receptor activity. In human, it is usually composed of either two alpha, two beta and one gamma chain of the GABA-A receptor subunits or 5 chains of the GABA-A receptor subunits rho1-3 (formally known as GABA-C receptor). [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:18790874]
chloride channel complexcellular componentAn ion channel complex through which chloride ions pass. [GOC:mah]
GABA receptor complexcellular componentA protein complex which is capable of GABA receptor activity. Upon binding of gamma-aminobutyric acid (GABA) it transmits the signal from one side of the membrane to the other to initiate a change in cell activity. Major inhibitory receptor in vertebrate brain. Also found in other vertebrate tissues, invertebrates and possibly in plants. Effective benzodiazepine receptor. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:18790874]
transmembrane transporter complexcellular componentA transmembrane protein complex which enables the transfer of a substance from one side of a membrane to the other. [GOC:bhm, GOC:TermGenie, PMID:18024586]

Involved In

This protein is involved in 5 target(s):

TargetCategoryDefinition
gamma-aminobutyric acid signaling pathwaybiological processThe series of molecular signals generated by the binding of gamma-aminobutyric acid (GABA, 4-aminobutyrate), an amino acid which acts as a neurotransmitter in some organisms, to its receptor on the surface of a target cell. [GOC:mah]
synaptic transmission, GABAergicbiological processThe vesicular release of gamma-aminobutyric acid (GABA). from a presynapse, across a chemical synapse, the subsequent activation of GABA receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, ISBN:0126603030]
chloride transmembrane transportbiological processThe process in which chloride is transported across a membrane. [GOC:TermGenie, GOC:vw]
inhibitory synapse assemblybiological processThe aggregation, arrangement and bonding together of a set of components to form an inhibitory synapse. [GO_REF:0000079, GOC:bf, GOC:PARL, GOC:TermGenie]
regulation of postsynaptic membrane potentialbiological processAny process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef]