General Information of the Protein
Protein ID
PT02002
Protein Name
Gamma-aminobutyric acid receptor subunit alpha-5
Secondarily
Protein Name
GABA(A) receptor subunit alpha-5
Gene Name
GABRA5
Sequence
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGYDNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPLNNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDFPMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTSTGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAAKIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYNSISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
GABA-A receptor
Function
Ligand-gated chloride channel subunit which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain (PubMed:29961870, PubMed:31056671). May be involved in GABA-A receptor assembly, and GABA-A receptor immobilization and accumulation by gephyrin at the synapse (PubMed:31056671).
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Uniprot ID
Primary ID:
P31644

Secondarily ID:
A8K338
Q14DC2
Q53XL6
Q9NYT3
Q9NYT4
Q9NYT5
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HGNC ID
HGNC:4079
Subcellular Location
Postsynaptic cell membrane
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0551322
US8778932, 36
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C19H12FN3O2S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0379892
US8778932, 6
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C19H13N3O2S
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0526532
US8778932, 21
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C19H12FN3O2S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0569564
US8778932, 9
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C20H11ClF3N3O2S
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0412460
US8778932, 31
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C20H12F3N3O2S
 1
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0000163
Ambien
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C19H21N3O
 1
1 EC50 > 3000 nM
CP0000619
RO-154513
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C15H14N6O3
 1
1 Kd = 3.8 nM
Clinical Information about the Protein
Target 1 ( GABA(A) receptor alpha-5 (GABRA5) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Benzodiazepine overdose [ICD-11: PC91]
2 Alzheimer disease [ICD-11: 8A20]
3 Inflammatory bowel disease [ICD-11: DD72]
4 Inflammation [ICD-11: 1A00-CA43.1]
Approved Drug(s) 1 Approved Drug  1
1 Flumazenil Approved
Benzodiazepine overdose
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Basmisanil Phase 2
Alzheimer disease
2 GSK683699 Phase 2
Inflammatory bowel disease
Investigative Drug(s) 1 Investigative Drug  1
1 [3H]CGS8216 Investigative
Inflammation
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT03373 Gamma-aminobutyric acid receptor subunit alpha-3 Homo sapiens, Human