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

GABRD (O14764) - Overview - Molecular Target Synopsis

Protein


GABRD, Gamma-aminobutyric acid receptor subunit delta
UniProt O14764

Also Known as GBRD_HUMAN, GABRD

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
452ENSG00000187730ENST00000378585ENSP00000367848O14764-1

Drugs


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

Sub-cellular localization


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



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRD has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HCT_116, SNB_19, LOXIMVI

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC12, MDA-MB-134-VI, NCI-H2198

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 GABRD there are:
6 structures (14 chains) solved
4 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRD has been screened with 643 compounds (851 bioactivities), 267 compounds have bioactivities that show binding affinity of <= 500nM (324 bioactivities). (see details)