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

GABRG1 (Q8N1C3) - Overview - Molecular Target Synopsis

Protein


GABRG1, Gamma-aminobutyric acid receptor subunit gamma-1
UniProt Q8N1C3

Also Known as GBRG1_HUMAN, GABRG1

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
465ENSG00000163285ENST00000295452ENSP00000295452Q8N1C3-1

Drugs


GABRG1 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)
Ethchlorvynol
Clobazam
Eszopiclone

Sub-cellular localization


UniProt: GABRG1 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRG1 is active in the following subcellular-locations: cell junction, chloride channel complex, dendrite membrane, GABA-A receptor complex, integral component of plasma membrane, neuron projection, postsynapse, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRG1 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: HS578T, MCF7, TK_10

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: CPC-N, KMS-27, SK-MM-2

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 GABRG1 there are:
10 structures (10 chains) solved
8 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRG1 has been screened with 643 compounds (853 bioactivities), 267 compounds have bioactivities that show binding affinity of <= 500nM (324 bioactivities). (see details)