Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

GABRA3 (P34903) - Overview - Molecular Target Synopsis

Protein


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

Drugs


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

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.



UniProt
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):

FYP/FLUMAZENIL (6D6T_D, 6D6U_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRA3 has been screened with 1463 compounds (2383 bioactivities), 860 compounds have bioactivities that show binding affinity of <= 500nM (1109 bioactivities). (see details)