Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

GABRA3 (P34903) - Overview - Molecular Target Synopsis


GABRA3, Gamma-aminobutyric acid receptor subunit alpha-3
UniProt P34903

Also Known as GBRA3_HUMAN, GABRA3

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Generally pentameric. There are five types of GABA(A) receptor chains: alpha, beta, gamma, delta, and rho. Binds UBQLN1 (By similarity). Interacts with GPHN (PubMed:26613940).

Isoforms / Transcripts (Protein Coding)

Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
492ENSG00000011677ENST00000535043, ENST00000370314ENSP00000443527, ENSP00000359337P34903-1


GABRA3 is targeted by Approved Drugs Eszopiclone, Ethchlorvynol, Methohexital, Clobazam. (see details)

Sub-cellular localization

UniProt: GABRA3 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRA3 is active in the following subcellular-locations: cell junction, chloride channel complex, dendrite membrane, GABA-A receptor complex, GABA-ergic synapse, integral component of plasma membrane, integral component of postsynaptic specialization membrane, neuron projection, plasma membrane, postsynapse, synapse.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project GABRA3 has gain in 1 cell-lines, loss in 20 cell-lines and no signal in 984 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: MCF7, HL_60, SK_MEL_5

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H520, G28T, G59

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, HSMM, HMEC

(see details)

3D Structures

At greater than 75% identity similarity to GABRA3 there are:
5 structures (9 chains) solved
5 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

GABRA3 is solved in complex with the approved drug(s):


(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

GABRA3 has been screened with 1481 compounds (2425 bioactivities), 865 compounds have bioactivities that show binding affinity of <= 500nM (1116 bioactivities). (see details)