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

GABRA4 (P48169) - Overview - Molecular Target Synopsis

Protein


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
554ENSG00000109158ENST00000264318ENSP00000264318P48169-1
36ENSG00000109158ENST00000502874ENSP00000424386

Drugs


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

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.



UniProt
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
4 are solved with an approved drug

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

FYP/FLUMAZENIL (6D6T_D, 6D6U_D),
08H/ALPRAZOLAM (6HUO_D),
DZP/DIAZEPAM (6HUP_D).

(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)