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

GABRQ (Q9UN88) - Overview - Molecular Target Synopsis

Protein


GABRQ, Gamma-aminobutyric acid receptor subunit theta
UniProt Q9UN88

Also Known as GBRT_HUMAN, GABRQ

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. This subunit coassembles with alpha-2, beta-1 and gamma-1.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
632ENSG00000147402ENST00000370306ENSP00000359329Q9UN88-1

Drugs


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

Sub-cellular localization


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



UniProt
GO terms

Gene Copy Number Variation


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

Gene Expression


In NCI60, the highest expressing cell lines are: LOXIMVI, HOP_62, SNB_19

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G121, UKE-1, 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: SK-N-SH, NHLF, HSMM

(see details)

3D Structures


At greater than 50% identity similarity to GABRQ there are:
14 structures (35 chains) solved
12 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

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

DZP/DIAZEPAM (6HUP_B, 6HUP_E).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRQ has been screened with 642 compounds (850 bioactivities), 267 compounds have bioactivities that show binding affinity of <= 500nM (324 bioactivities). (see details)