Proteins > Gamma-aminobutyric acid receptor subunit delta
Page last updated: 2024-08-07 15:22:18
Gamma-aminobutyric acid receptor subunit delta
A gamma-aminobutyric acid receptor subunit delta that is encoded in the genome of human. [PRO:DNx, UniProtKB:O14764]
Synonyms
GABA(A) receptor subunit delta
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (12.50) | 18.7374 |
| 1990's | 6 (25.00) | 18.2507 |
| 2000's | 10 (41.67) | 29.6817 |
| 2010's | 4 (16.67) | 24.3611 |
| 2020's | 1 (4.17) | 2.80 |
Compounds (70)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gamma-aminobutyric acid | Homo sapiens (human) | Ki | 0.1165 | 2 | 2 |
| phenytoin | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| clonazepam | Homo sapiens (human) | IC50 | 555,904.0000 | 1 | 1 |
| clonazepam | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| nordazepam | Homo sapiens (human) | IC50 | 106,414.0000 | 1 | 1 |
| diazepam | Homo sapiens (human) | IC50 | 41,198.3400 | 3 | 3 |
| diazepam | Homo sapiens (human) | Ki | 0.0100 | 2 | 2 |
| fipronil | Homo sapiens (human) | IC50 | 0.0023 | 1 | 1 |
| flumazenil | Homo sapiens (human) | Ki | 0.0009 | 2 | 2 |
| flunitrazepam | Homo sapiens (human) | IC50 | 263,027.0000 | 1 | 1 |
| fluoxetine | Homo sapiens (human) | IC50 | 5.2000 | 1 | 2 |
| hydroxyurea | Homo sapiens (human) | Ki | 113.0000 | 1 | 2 |
| isoguvacine | Homo sapiens (human) | Ki | 0.0550 | 1 | 2 |
| 4-piperidinecarboxylic acid | Homo sapiens (human) | Ki | 0.5056 | 1 | 2 |
| muscimol | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| muscimol | Homo sapiens (human) | Ki | 0.0085 | 2 | 2 |
| nitrazepam | Homo sapiens (human) | IC50 | 100,000.0000 | 1 | 1 |
| cm 7116 | Homo sapiens (human) | IC50 | 500,035.0000 | 1 | 1 |
| temazepam | Homo sapiens (human) | IC50 | 62,517.3000 | 1 | 1 |
| triiodothyronine | Homo sapiens (human) | IC50 | 23.0000 | 1 | 1 |
| bicuculline | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| flavone | Homo sapiens (human) | Ki | 0.5085 | 2 | 2 |
| chlordesmethyldiazepam | Homo sapiens (human) | IC50 | 277,952.0014 | 2 | 2 |
| 6-aminonicotinic acid | Homo sapiens (human) | Ki | 4.2369 | 1 | 2 |
| halazepam | Homo sapiens (human) | IC50 | 10,864.3000 | 1 | 1 |
| progabide | Homo sapiens (human) | Ki | 40.0000 | 1 | 1 |
| duloxetine | Homo sapiens (human) | IC50 | 0.0190 | 1 | 2 |
| norharman | Homo sapiens (human) | IC50 | 1.6218 | 1 | 1 |
| baicalin | Homo sapiens (human) | Ki | 77.6247 | 1 | 1 |
| 2-aminonicotinic acid | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| n-desmethylflunitrazepam | Homo sapiens (human) | IC50 | 25,003.5000 | 1 | 1 |
| 7-aminonitrazepam | Homo sapiens (human) | IC50 | 2,588.2100 | 1 | 1 |
| ro 20-1815 | Homo sapiens (human) | IC50 | 15,381.5000 | 1 | 1 |
| brexanolone | Homo sapiens (human) | IC50 | 0.0220 | 1 | 1 |
| 2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-one | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| beta-carboline-3-carboxylic acid ethyl ester | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| beta-carboline-3-carboxylic acid methyl ester | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| 3-ethoxy-beta-carboline | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| tert-butyl beta-carboline-3-carboxylate | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| 3',6-dinitroflavone | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| cgp 36742 | Homo sapiens (human) | IC50 | 508.0000 | 1 | 1 |
| pitrazepin | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| 7-aminoclonazepam | Homo sapiens (human) | IC50 | 13,335.2000 | 1 | 1 |
| ro 5-3438 | Homo sapiens (human) | IC50 | 71,449.6000 | 1 | 1 |
| cocaine | Homo sapiens (human) | IC50 | 127.0000 | 1 | 1 |
| 6-bromoflavone | Homo sapiens (human) | Ki | 0.0708 | 1 | 1 |
| n-desmethylflunitrazepam | Homo sapiens (human) | IC50 | 666,807.0000 | 1 | 1 |
| ro 05-4082 | Homo sapiens (human) | IC50 | 454,988.0000 | 1 | 1 |
| l 364373 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 1-(1h-indol-3-ylcarbonyl)-n-(4-methoxybenzyl)formamide | Homo sapiens (human) | Ki | 0.1622 | 1 | 1 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | IC50 | 0.0110 | 1 | 2 |
| meclonazepam | Homo sapiens (human) | IC50 | 833,681.0000 | 1 | 1 |
| isothaz | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| n-(indol-3-ylglyoxylyl)benzylamine | Homo sapiens (human) | Ki | 0.1202 | 1 | 1 |
| 6-bromo-3'-nitroflavone | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| 3-propoxy-beta-carboline | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| apigenin | Homo sapiens (human) | Ki | 3.0200 | 1 | 1 |
| harman | Homo sapiens (human) | IC50 | 12.3027 | 1 | 1 |
| amentoflavone | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| baicalein | Homo sapiens (human) | Ki | 5.6234 | 1 | 1 |
| chrysin | Homo sapiens (human) | Ki | 3.0200 | 1 | 1 |
| hispidulin | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| scutellarein | Homo sapiens (human) | Ki | 12.0226 | 1 | 1 |
| wogonin | Homo sapiens (human) | Ki | 2.0417 | 1 | 1 |
| 1-Ethyl-9H-pyrido[3,4-b]indole | Homo sapiens (human) | IC50 | 251.1890 | 1 | 1 |
| ganaxolone | Homo sapiens (human) | IC50 | 0.0420 | 1 | 1 |
| bis(7)-tacrine | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| basimglurant | Homo sapiens (human) | Ki | 3.1600 | 1 | 1 |
| ro 4956371 | Homo sapiens (human) | Ki | 3.1600 | 1 | 1 |
| mdv 3100 | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| valproate sodium | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| apalutamide | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| brexanolone | Homo sapiens (human) | EC50 | 0.0755 | 1 | 1 |
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones.Journal of medicinal chemistry, , Volume: 25, Issue:9, 1982
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.Journal of medicinal chemistry, , Volume: 23, Issue:6, 1980
3D-QSAR model of flavonoids binding at benzodiazepine site in GABAA receptors.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Mixture-based synthetic combinatorial libraries.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones.Journal of medicinal chemistry, , Volume: 25, Issue:9, 1982
Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential | molecular function | Any transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
| GABA-A receptor activity | molecular function | Combining 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] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
| GABA-ergic synapse | cellular component | A synapse that uses GABA as a neurotransmitter. These synapses are typically inhibitory. [GOC:dos] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synapse | cellular component | The 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 projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| GABA-A receptor complex | cellular component | A 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 complex | cellular component | An ion channel complex through which chloride ions pass. [GOC:mah] |
| transmembrane transporter complex | cellular component | A 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 7 target(s):
| Target | Category | Definition |
|---|
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| gamma-aminobutyric acid signaling pathway | biological process | The 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, GABAergic | biological process | The 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] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| chloride transmembrane transport | biological process | The process in which chloride is transported across a membrane. [GOC:TermGenie, GOC:vw] |
| regulation of membrane potential | biological process | Any process that modulates the establishment or extent of a membrane potential, the electric potential existing across any membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:jl, GOC:mtg_cardio, GOC:tb, ISBN:0198506732] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter 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:jl, MeSH:D009435] |