Details of the Target

General Information of Target

Target ID LDTP00320
Target Name Gamma-aminobutyric acid receptor subunit pi (GABRP)
Gene Name GABRP
Gene ID 2568
Synonyms
Gamma-aminobutyric acid receptor subunit pi; GABA(A) receptor subunit pi
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNYSLHLAFVCLSLFTERMCIQGSQFNVEVGRSDKLSLPGFENLTAGYNKFLRPNFGGEP
VQIALTLDIASISSISESNMDYTATIYLRQRWMDQRLVFEGNKSFTLDARLVEFLWVPDT
YIVESKKSFLHEVTVGNRLIRLFSNGTVLYALRITTTVACNMDLSKYPMDTQTCKLQLES
WGYDGNDVEFTWLRGNDSVRGLEHLRLAQYTIERYFTLVTRSQQETGNYTRLVLQFELRR
NVLYFILETYVPSTFLVVLSWVSFWISLDSVPARTCIGVTTVLSMTTLMIGSRTSLPNTN
CFIKAIDVYLGICFSFVFGALLEYAVAHYSSLQQMAAKDRGTTKEVEEVSITNIINSSIS
SFKRKISFASIEISSDNVDYSDLTMKTSDKFKFVFREKMGRIVDYFTIQNPSNVDHYSKL
LFPLIFMLANVFYWAYYMYF
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Ligand-gated ion channel (TC 1.A.9) family, Gamma-aminobutyric acid receptor (TC 1.A.9.5) subfamily, GABRP sub-subfamily
Subcellular location
Postsynaptic cell membrane
Function
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.
TTD ID
T49208
Uniprot ID
O00591
DrugMap ID
TT3E0DI
Ensemble ID
ENST00000265294.9
HGNC ID
HGNC:4089
ChEMBL ID
CHEMBL2093872

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
CY-1
 Probe Info  		Q235(0.00); R239(0.00)  LDD0246  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 30 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amoxapine Small molecular drug DB00543
Apalutamide Small molecular drug DB11901
Butabarbital Small molecular drug DB00237
Butalbital Small molecular drug DB00241
Clonazepam Small molecular drug DB01068
Desflurane Small molecular drug DB01189
Enflurane Small molecular drug DB00228
Eszopiclone Small molecular drug DB00402
Ethanol Small molecular drug DB00898
Etomidate Small molecular drug DB00292
Flumazenil Small molecular drug DB01205
Glutethimide Small molecular drug DB01437
Halothane Small molecular drug DB01159
Isoflurane Small molecular drug DB00753
Lamotrigine Small molecular drug DB00555
Medroxyprogesterone Acetate Small molecular drug DB00603
Memantine Small molecular drug DB01043
Meprobamate Small molecular drug DB00371
Methoxyflurane Small molecular drug DB01028
Methyprylon Small molecular drug DB01107
Nitrazepam Small molecular drug DB01595
Pentobarbital Small molecular drug DB00312
Phenytoin Small molecular drug DB00252
Prasterone Small molecular drug DB01708
Primidone Small molecular drug DB00794
Propofol Small molecular drug DB00818
Sevoflurane Small molecular drug DB01236
Stiripentol Small molecular drug DB09118
Talbutal Small molecular drug DB00306
Taurine Small molecular drug DB01956
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tbps Small molecular drug D0P0TI
Thiocolchicoside Small molecular drug DB11582
Etizolam . DB09166
Discontinued
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fludiazepam Small molecular drug DB01567
Metharbital Small molecular drug DB00463

References

1 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.