General Information of the Protein
Protein ID
PT03372
Protein Name
Gamma-aminobutyric acid receptor subunit alpha-2
Secondarily
Protein Name
GABA(A) receptor subunit alpha-2
Gene Name
GABRA2
Sequence
MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPGLGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSCPLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASVMIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRMSRIVFPVLFGTFNLVYWATYLNREPVLGVSP
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Ligand-gated ion channel
>
GABA-A receptor
Function
Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain (PubMed:29961870, PubMed:31032849). Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel (PubMed:29961870, PubMed:31032849). The gamma2 subunit is necessary but not sufficient for a rapid formation of active synaptic contacts and the synaptogenic effect of this subunit is influenced by the type of alpha and beta subunits present in the receptor pentamer (By similarity). The alpha2/beta2/gamma2 receptor exhibits synaptogenic activity whereas the alpha2/beta3/gamma2 receptor shows very little or no synaptogenic activity (By similarity).
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Uniprot ID
Primary ID:
P47869

Secondarily ID:
A8K0U7
B7Z1H8
Q59G14
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HGNC ID
HGNC:4076
Subcellular Location
Postsynaptic cell membrane
Cell membrane
Cytoplasmic vesicle membrane
Cell projection
Dendrite
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: CL000011 , CHO
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0471857
 Compound Info 
3-(2-chlorobenzyloxy)-2-(2-fluorophenyl)-2H-pyrazolo[4,3-c]quinoline
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C23H15ClFN3O
  1
1
IC50 = 2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0806010
 Compound Info 
2-(4-chlorophenyl)-2H-pyrazolo[4,3-c]quinolin-3(5H)-one
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C16H10ClN3O
  1
1
IC50 = 4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0489251
 Compound Info 
2-(4-chlorophenyl)-3-(4-fluorobenzyloxy)-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C23H19ClFN3O
  1
1
IC50 = 57 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0381663
 Compound Info 
2-(4-chlorophenyl)-3-(2-fluorobenzyloxy)-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C23H19ClFN3O
  1
1
IC50 = 154 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0469122
 Compound Info 
2-(benzo[d][1,3]dioxol-5-yl)-3-(2-chlorobenzyloxy)-2H-pyrazolo[4,3-c]quinoline
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C24H16ClN3O3
  1
1
IC50 = 155 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0381662
 Compound Info 
3-(4-chlorobenzyloxy)-2-(4-chlorophenyl)-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C23H19Cl2N3O
  1
1
IC50 = 177 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0492329
 Compound Info 
2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C20H20ClN3O
  1
1
IC50 = 185 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0381664
 Compound Info 
3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-8,8-dimethyl-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C25H23Cl2N3O
  1
1
IC50 = 213 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0471840
 Compound Info 
3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-2H-pyrazolo[4,3-c]quinoline
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C23H15Cl2N3O
  1
1
IC50 = 265 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0502352
 Compound Info 
3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C23H19Cl2N3O
  1
1
IC50 = 271 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0469121
 Compound Info 
3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-2,6,7,9-tetrahydropyrano[4,3-b]pyrazolo[3,4-d]pyridine
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C22H17Cl2N3O2
  1
1
IC50 = 461 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0471858
 Compound Info 
2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-2H-pyrazolo[4,3-c]quinoline
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C20H16ClN3O
  1
1
IC50 = 472 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0480355
 Compound Info 
3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-2,6,7,8,9,10-hexahydrocyclohepta[b]pyrazolo[3,4-d]pyridine
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C24H21Cl2N3O
  1
1
IC50 = 605 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0504403
 Compound Info 
2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-8-(1H-imidazol-1-yl)-2H-pyrazolo[4,3-c]quinoline
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C23H18ClN5O
  1
1
IC50 = 2114 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0505700
 Compound Info 
3-(2-chlorophenoxy)-2-(4-chlorophenyl)-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline
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C22H17Cl2N3O
  1
1
IC50 > 3000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Clinical Information about the Protein
Target 1 ( GABA(A) receptor alpha-2 (GABRA2) )
Target Type Successful Target
Disease 4 Target-related Diseases  4
1 Benzodiazepine overdose [ICD-11: PC91]
2 Inflammatory bowel disease [ICD-11: DD72]
3 Alcohol dependence [ICD-11: 6C40.2]
4 Inflammation [ICD-11: 1A00-CA43.1]
Approved Drug(s) 1 Approved Drug  1
1 Flumazenil
 Drug Info 
Approved
Benzodiazepine overdose
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 GSK683699
 Drug Info 
Phase 2
Inflammatory bowel disease
Discontinued Drug(s) 1 Discontinued Drug  1
1 CGS-17867A
 Drug Info 
Terminated
Alcohol dependence
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
PT05269 Gamma-aminobutyric acid receptor subunit alpha-2 Rattus norvegicus, Rat
 Protein Info