General Information of the Protein
Protein ID
PT05269
Protein Name
Gamma-aminobutyric acid receptor subunit alpha-2
Secondarily
Protein Name
GABA(A) receptor subunit alpha-2
Gene Name
GABRA2
Secondarily
Gene Name
Gabra-2
Sequence
MRTKLSTCNVWFPLLVLLVWNPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPGLGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNSMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSCPLKFGSYAYTTSEVTYIWTYNPSDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKGSVMIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRMSRIVFPVLFGTFNLVYWATYLNREPVLGVSP
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Organism
Rattus norvegicus, Rat
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 (By similarity). Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel (By similarity). 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
P23576
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0000099
7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
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C16H13ClN2O
 1
1
Ki = 15 nM
   TI
   LI
   LO
   TS
CP0000229
(R)-N-(2,3-dihydro-1H-inden-1-yl)-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide
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C19H15N3O4
 1
1
Ki = 85 nM
   TI
   LI
   LO
   TS
CP0003479
N-[(4-fluorophenyl)methyl]-2-(1H-indol-3-yl)-2-oxoacetamide
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C17H13FN2O2
 1
1
Ki = 118 nM
   TI
   LI
   LO
   TS
CP0003771
(R)-2-(5-nitro-1H-indol-3-yl)-2-oxo-N-(1-phenylethyl)acetamide
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C18H15N3O4
 1
1
Ki = 121 nM
   TI
   LI
   LO
   TS
CP0002470
2-(1H-Indol-3-yl)-N-(4-nitro-benzyl)-2-oxo-acetamide
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C17H13N3O4
 1
1
Ki = 210 nM
   TI
   LI
   LO
   TS
CP0010590
(R/S)-N-(5-methoxy-2,3-dihydro-1H-inden-1-yl)-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide
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C20H17N3O5
 1
1
Ki = 231 nM
   TI
   LI
   LO
   TS
CP0009202
(R/S)-2-(5-nitro-1H-indol-3-yl)-N-(5-nitro-2,3-dihydro-1H-inden-1-yl)-2-oxoacetamide
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C19H14N4O6
 1
1
Ki = 513 nM
   TI
   LI
   LO
   TS
CP0002158
(R/S)-2-(1H-indol-3-yl)-N-(5-methoxy-2,3-dihydro-1H-inden-1-yl)-2-oxoacetamide
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C20H18N2O3
 1
1
Ki = 690 nM
   TI
   LI
   LO
   TS
CP0000163
Ambien
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C19H21N3O
 1
1
Ki = 765 nM
   TI
   LI
   LO
   TS
CP0009201
(R/S)-N-(5-fluoro-2,3-dihydro-1H-inden-1-yl)-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide
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C19H14FN3O4
 1
1
Ki = 810 nM
   TI
   LI
   LO
   TS
CP0004581
(R)-2-(1H-indol-3-yl)-2-oxo-N-(1-phenylethyl)acetamide
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C18H16N2O2
 1
1
Ki = 1550 nM
   TI
   LI
   LO
   TS
CP0002684
N-[(4-methoxyphenyl)methyl]-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide
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C18H15N3O5
 1
1
Ki = 1645 nM
   TI
   LI
   LO
   TS
CP0009784
2-(1H-Indol-3-yl)-N-(4-methoxy-benzyl)-2-oxo-acetamide
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C18H16N2O3
 1
1
Ki = 1950 nM
   TI
   LI
   LO
   TS
CP0000228
2-(5-nitro-1H-indol-3-yl)-N-(4-nitrobenzyl)-2-oxoacetamide
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C17H12N4O6
 1
1
Ki = 2980 nM
   TI
   LI
   LO
   TS
CP0002157
(R)-N-(2,3-dihydro-1H-inden-1-yl)-2-(1H-indol-3-yl)-2-oxoacetamide
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C19H16N2O2
 1
1
Ki = 3100 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT03372 Gamma-aminobutyric acid receptor subunit alpha-2 Homo sapiens, Human