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

GABRA5 (P31644) - Overview - Molecular Target Synopsis

Protein


GABRA5, Gamma-aminobutyric acid receptor subunit alpha-5
UniProt P31644

Also Known as GBRA5_HUMAN, GABRA5

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.

6A96
CRYO-EM STRUCTURE OF THE HUMAN ALPHA5BETA3 GABAA RECEPTOR IN COMPLEX WITH GABA AND NB25
RCSB/PDB
Inspect Structure
See all 3D Structures for GABRA5

Isoforms / Transcripts (Protein Coding)


Drugs


GABRA5 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)
Ethchlorvynol
Clobazam
Eszopiclone

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRA5 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: A549, UACC_257, SF_268

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: A549, NCI-N417, DMS 273

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: A549, SK-N-SH, NHLF

(see details)

3D Structures


For GABRA5 there are:
3 structures (11 chains) solved
3 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRA5 has been screened with 1825 compounds (2690 bioactivities), 1261 compounds have bioactivities that show binding affinity of <= 500nM (1505 bioactivities). (see details)