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

GABRG3 (Q99928) - Overview - Molecular Target Synopsis

Protein


GABRG3, Gamma-aminobutyric acid receptor subunit gamma-3
UniProt Q99928

Also Known as GBRG3_HUMAN, GABRG3

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)


Drugs


GABRG3 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)
Ethchlorvynol
Clobazam
Eszopiclone

Sub-cellular localization


UniProt: GABRG3 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRG3 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 synaptic membrane, neuron projection, plasma membrane, postsynapse, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRG3 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, NCI_H460, TK_10

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC12, NCI-H1155, DMS 79

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 GABRG3 there are:
2 structures (2 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRG3 has been screened with 643 compounds (853 bioactivities), 267 compounds have bioactivities that show binding affinity of <= 500nM (324 bioactivities). (see details)