Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

GABRP (O00591) - Overview - Molecular Target Synopsis


GABRP, Gamma-aminobutyric acid receptor subunit pi
UniProt O00591


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. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone. Generally pentameric. There are five types of GABA(A) receptor chains: alpha, beta, gamma, delta, and epsilon. A sixth class of subunit: Rho form homomeric GABA receptors that do not appear to coexist with GABA(A) receptor subunits but with GABA(C) receptor subunits. Subunit Pi can also bind this complex.

Isoforms / Transcripts (Protein Coding)


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

Sub-cellular localization

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

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project GABRP has gain in 2 cell-lines, loss in 2 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: NCI_H322M, HT29, RXF_393

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Calu-3, H322T, HCC1143

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: MCF-7, SK-N-SH, NHLF

(see details)

3D Structures

At greater than 50% identity similarity to GABRP there are:
10 structures (33 chains) solved
8 are solved in complex with at least one small molecule ligand

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

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