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

GABRA4 (P48169) - Overview - Molecular Target Synopsis


GABRA4, Gamma-aminobutyric acid receptor subunit alpha-4
UniProt P48169

Also Known as GBRA4_HUMAN, GABRA4

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.

Isoforms / Transcripts (Protein Coding)

Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform


GABRA4 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)

Sub-cellular localization

UniProt: GABRA4 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRA4 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 GABRA4 has gain in 0 cell-lines, loss in 4 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: SF_295, SNB_19, SN12C

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, LN-18

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: SK-N-SH, NHLF, HSMM

(see details)

3D Structures

At greater than 50% identity similarity to GABRA4 there are:
16 structures (48 chains) solved
13 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

GABRA4 is solved in complex with the approved drug(s):


(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

GABRA4 has been screened with 795 compounds (1126 bioactivities), 298 compounds have bioactivities that show binding affinity of <= 500nM (387 bioactivities). (see details)