General Information of the Protein
Protein ID
PT05027
Protein Name
Gamma-aminobutyric acid receptor subunit beta-3
Secondarily
Protein Name
GABA(A) receptor subunit beta-3
Gene Name
GABRB3
Sequence
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPPVCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNRVDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRSLPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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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:18514161, PubMed:22303015, PubMed:26950270, PubMed:22243422, PubMed:24909990). 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:25489750). 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 alpha1/beta3/gamma2 receptor exhibits synaptogenic activity (PubMed:25489750). The alpha2/beta3/gamma2 receptor shows very little or no synaptogenic activity (By similarity). Functions also as histamine receptor and mediates cellular responses to histamine (PubMed:18281286). Plays an important role in somatosensation and in the production of antinociception (By similarity).
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Uniprot ID
Primary ID:
P28472

Secondarily ID:
B7Z2W1
B7Z825
F5H3D2
H7BYV8
Q14352
Q96FM5
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HGNC ID
HGNC:4083
Subcellular Location
Postsynaptic cell membrane
Cell membrane
Cytoplasmic vesicle 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
CP0006347
5-chloromethyl-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-n-propyl-1H-1,2,3-triazole
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C13H11Cl3F3N3
 1
1
Ki = 0.659 nM
   TI
   LI
   LO
   TS
CP0005753
1-(2,6-dichloro-4-trifluoromethylphenyl)-5-methyl-4-n-propyl-1H-1,2,3-triazole
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C13H12Cl2F3N3
 1
1
Ki = 1.94 nM
   TI
   LI
   LO
   TS
CP0004022
1-(2,6-dichloro-4-trifluoromethylphenyl)-5-hydroxymethyl-4-n-propyl-1H-1,2,3-triazole
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C13H12Cl2F3N3O
 1
1
Ki = 2.53 nM
   TI
   LI
   LO
   TS
CP0004023
1-(2,6-dichloro-4-trifluoromethylphenyl)-4,5-diethyl-1H-1,2,3-triazole
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C13H12Cl2F3N3
 1
1
Ki = 4.27 nM
   TI
   LI
   LO
   TS
CP0006914
1-(2,6-dichloro-4-trifluoromethylphenyl)-4-ethyl-5-methyl-1H-1,2,3-triazole
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C12H10Cl2F3N3
 1
1
Ki = 7.08 nM
   TI
   LI
   LO
   TS
CP0009680
1-(2,6-dichloro-4-trifluoromethylphenyl)-5-ethyl-4-n-propyl-1H-1,2,3-triazole
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C14H14Cl2F3N3
 1
1
Ki = 8.07 nM
   TI
   LI
   LO
   TS
CP0000270
1-(2,6-dibromo-4-trifluoromethylphenyl)-5-methyl-4-n-propyl-1H-1,2,3-triazole
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C13H12Br2F3N3
 1
1
Ki = 13.6 nM
   TI
   LI
   LO
   TS
CP0011540
1-(2,6-dichloro-4-trifluoromethylphenyl)-4-ethyl-5-n-propyl-1H-1,2,3-triazole
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C14H14Cl2F3N3
 1
1
Ki = 47.2 nM
   TI
   LI
   LO
   TS
CP0005242
4-chloromethyl-1-(2,6-dichloro-4-trifluoromethylphenyl)-5-n-propyl-1H-1,2,3-triazole
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C13H11Cl3F3N3
 1
1
Ki = 66.7 nM
   TI
   LI
   LO
   TS
CP0009681
1-(2,6-dichloro-4-(trifluoromethyl)phenyl)-5-ethyl-4-methyl-1H-1,2,3-triazole
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C12H10Cl2F3N3
 1
1
Ki = 70.1 nM
   TI
   LI
   LO
   TS
CP0009679
1-(2,6-dichloro-4-trifluoromethylphenyl)-4,5-di-npropyl-1H-1,2,3-triazole
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C15H16Cl2F3N3
 1
1
Ki = 128 nM
   TI
   LI
   LO
   TS
CP0013392
1-(2,6-dichloro-4-trifluoromethylphenyl)-4-methyl-5-n-propyl-1H-1,2,3-triazole
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C13H12Cl2F3N3
 1
1
Ki = 539 nM
   TI
   LI
   LO
   TS
CP0014069
1-(2,6-dichloro-4-trifluoromethylphenyl)-4-hydroxymethyl-5-n-propyl-1H-1,2,3-triazole
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C13H12Cl2F3N3O
 1
1
Ki = 3450 nM
   TI
   LI
   LO
   TS