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

GABRR3 (A8MPY1) - Overview - Molecular Target Synopsis

Protein


GABRR3, Gamma-aminobutyric acid receptor subunit rho-3
UniProt A8MPY1

Also Known as GBRR3_HUMAN, GABRR3

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. Forms a ternary complex with SQSTM1 and PRKCZ.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
467A8MPY1-1
466ENSG00000183185ENST00000472788ENSP00000420790

Sub-cellular localization


UniProt: GABRR3 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRR3 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, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRR3 has gain in 2 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: TK_10, KM12, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, LN-18

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 GABRR3 there are:
1 structures (1 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRR3 has been screened with 16 compounds (19 bioactivities), 3 compounds have bioactivities that show binding affinity of <= 500nM (3 bioactivities). (see details)