General Information of the Protein
Protein ID
PT03373
Protein Name
Gamma-aminobutyric acid receptor subunit alpha-3
Secondarily
Protein Name
GABA(A) receptor subunit alpha-3
Gene Name
GABRA3
Sequence
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDSTDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQTWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLLYTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRLNQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGAAPSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVNRESAIKGMIRKQ
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
GABA-A receptor
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.
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Uniprot ID
Primary ID:
P34903

Secondarily ID:
Q8TAF9
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Ensembl ID
ENSG00000011677
HGNC ID
HGNC:4077
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0000200
 Compound Info 
ethyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
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C17H15N3O3
  1
1
Ki = 25.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0008001
 Compound Info 
ethyl 12-ethynyl-9-phenyl-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene-5-carboxylate
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C22H17N3O2
  1
1
Ki = 96 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0002342
 Compound Info 
3-({12-ethynyl-9-phenyl-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,8,10,12-hexaen-5-yl}carbonyloxy)propyl 12-ethynyl-9-phenyl-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene-5-carboxylate
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C43H30N6O4
  1
1
Ki = 272 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0002647
 Compound Info 
3-({12-ethynyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,10,12-pentaen-5-yl}carbonyloxy)propyl 12-ethynyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,11,13-pentaene-5-carboxylate
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C33H26N6O6
  1
1
Ki = 858 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0008002
 Compound Info 
XLi374, 5
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C32H24N6O7
  1
1
Ki = 1864 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0008003
 Compound Info 
5-({12-ethynyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,10,12-pentaen-5-yl}carbonyloxy)pentyl 12-ethynyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,11,13-pentaene-5-carboxylate
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C35H30N6O6
  1
1
Ki = 2666 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0008395
 Compound Info 
3-({12-ethyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,10,12-pentaen-5-yl}carbonyloxy)propyl 12-ethyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,11,13-pentaene-5-carboxylate
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C33H34N6O6
  1
1
Ki = 8545 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( GABA(A) receptor alpha-3 (GABRA3) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Benzodiazepine overdose [ICD-11: PC91]
2 Inflammatory bowel disease [ICD-11: DD72]
3 Anxiety disorder [ICD-11: 6B00-6B0Z]
4 Schizophrenia [ICD-11: 6A20]
5 Inflammation [ICD-11: 1A00-CA43.1]
Approved Drug(s) 1 Approved Drug  1
1 Flumazenil
 Drug Info 
Approved
Benzodiazepine overdose
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 GSK683699
 Drug Info 
Phase 2
Inflammatory bowel disease
2 NS-2710
 Drug Info 
Phase 2
Anxiety disorder
Discontinued Drug(s) 1 Discontinued Drug  1
1 AZD6280
 Drug Info 
Discontinued in Phase 1
Schizophrenia
Investigative Drug(s) 1 Investigative Drug  1
1 [3H]CGS8216
 Drug Info 
Investigative
Inflammation
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02002 Gamma-aminobutyric acid receptor subunit alpha-5 Homo sapiens, Human
 Protein Info