Details of the Target

General Information of Target

Target ID LDTP03266
Target Name Gamma-aminobutyric acid receptor subunit rho-1 (GABRR1)
Gene Name GABRR1
Gene ID 2569
Synonyms
Gamma-aminobutyric acid receptor subunit rho-1; GABA(A) receptor subunit rho-1; GABA(C) receptor
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLAVPNMRFGIFLLWWGWVLATESRMHWPGREVHEMSKKGRPQRQRREVHEDAHKQVSPI
LRRSPDITKSPLTKSEQLLRIDDHDFSMRPGFGGPAIPVGVDVQVESLDSISEVDMDFTM
TLYLRHYWKDERLSFPSTNNLSMTFDGRLVKKIWVPDMFFVHSKRSFIHDTTTDNVMLRV
QPDGKVLYSLRVTVTAMCNMDFSRFPLDTQTCSLEIESYAYTEDDLMLYWKKGNDSLKTD
ERISLSQFLIQEFHTTTKLAFYSSTGWYNRLYINFTLRRHIFFFLLQTYFPATLMVMLSW
VSFWIDRRAVPARVPLGITTVLTMSTIITGVNASMPRVSYIKAVDIYLWVSFVFVFLSVL
EYAAVNYLTTVQERKEQKLREKLPCTSGLPPPRTAMLDGNYSDGEVNDLDNYMPENGEKP
DRMMVQLTLASERSSPQRKSQRSSYVSMRIDTHAIDKYSRIIFPAAYILFNLIYWSIFS
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, GABRR1 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. Rho-1 GABA receptor could play a role in retinal neurotransmission.
TTD ID
T99665
Uniprot ID
P24046
DrugMap ID
TT6XFEU
Ensemble ID
ENST00000369451.7
HGNC ID
HGNC:4090
ChEMBL ID
CHEMBL3561

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
GB1 SNV: p.P5L .
HCT15 SNV: p.P311H .
HEC1 SNV: p.K232R .
HT115 SNV: p.E35D .
HUH1 SNV: p.Y340F .
KNS42 SNV: p.D224N .
MEWO SNV: p.P90T .
NB1 SNV: p.W15R .
NCIH2291 SNV: p.A312D .
NUGC3 SNV: p.Y229S .
SUPT1 SNV: p.A343V .

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
CY4
 Probe Info  		N.A.  LDD0247  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lindane Small molecular drug DB00431
Investigative
Click To Hide/Show 11 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(+/-)-cis-2-camp Small molecular drug D0WV8K
5-me-iaa Small molecular drug D0C7PZ
Aza-thip Small molecular drug D0OY1R
Caca Small molecular drug D0O9UH
Cis-3-acpbpa Small molecular drug D0B0WU
Isonipecotic Acid Small molecular drug D0AC2H
Picrotoxin Small molecular drug DB00466
Piperidine-4-sulphonic Acid Small molecular drug D0VW5M
Tbps Small molecular drug D0P0TI
Tpmpa Small molecular drug D0U4HM
Trans-3-acpbpa Small molecular drug D0A6RM
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fludiazepam Small molecular drug DB01567

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.