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

GABRA2 (P47869) - Overview - Molecular Target Synopsis


GABRA2, Gamma-aminobutyric acid receptor subunit alpha-2
UniProt P47869

Also Known as GBRA2_HUMAN, GABRA2

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. Interacts with UBQLN1. Interacts with KIF21B. Interacts with LHFPL4.

Isoforms / Transcripts (Protein Coding)


GABRA2 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)

Sub-cellular localization

UniProt: GABRA2 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, cytoplasmic vesicle membrane, dendrite, postsynaptic cell membrane, synapse.
GO terms: GABRA2 is active in the following subcellular-locations: cell junction, chloride channel complex, dendrite membrane, GABA-A receptor complex, integral component of plasma membrane, integral component of synaptic vesicle membrane, neuron projection, plasma membrane, postsynapse, postsynaptic membrane, synapse.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project GABRA2 has gain in 0 cell-lines, loss in 6 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: SF_295, HOP_62, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: PSN1, Hs 675.T, SNU-182

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 75% identity similarity to GABRA2 there are:
13 structures (31 chains) solved
13 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

GABRA2 is solved in complex with the approved drug(s):


(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

GABRA2 has been screened with 1479 compounds (2257 bioactivities), 813 compounds have bioactivities that show binding affinity of <= 500nM (1066 bioactivities). (see details)