General Information of the Protein
Protein ID
PT03377
Protein Name
Gamma-aminobutyric acid receptor subunit alpha-1
Secondarily
Protein Name
GABA(A) receptor subunit alpha-1
Gene Name
GABRA1
Sequence
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
    Show/Hide
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:23909897, PubMed:25489750, PubMed:29950725). 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:23909897, 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/beta2/gamma2 receptor and the alpha1/beta3/gamma2 receptor exhibit synaptogenic activity (PubMed:23909897, PubMed:25489750). GABRA1-mediated plasticity in the orbitofrontal cortex regulates context-dependent action selection (By similarity). Functions also as histamine receptor and mediates cellular responses to histamine (By similarity).
    Show/Hide
Uniprot ID
Primary ID:
P14867

Secondarily ID:
D3DQK6
Q8N629
    Show/Hide
Ensembl ID
ENSG00000022355
HGNC ID
HGNC:4075
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: 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
   Show/Hide
C23H15ClFN3O
  1
1
IC50 = 1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0806010
 Compound Info 
2-(4-chlorophenyl)-2H-pyrazolo[4,3-c]quinolin-3(5H)-one
   Show/Hide
C16H10ClN3O
  1
1
IC50 = 1 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
   Show/Hide
C23H19Cl2N3O
  1
1
IC50 = 46 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
   Show/Hide
C24H16ClN3O3
  1
1
IC50 = 50 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
   Show/Hide
C23H19ClFN3O
  1
1
IC50 = 50 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
   Show/Hide
C23H19ClFN3O
  1
1
IC50 = 64 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0471840
 Compound Info 
3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-2H-pyrazolo[4,3-c]quinoline
   Show/Hide
C23H15Cl2N3O
  1
1
IC50 = 64 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
   Show/Hide
C25H23Cl2N3O
  1
1
IC50 = 67 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0471858
 Compound Info 
2-(4-chlorophenyl)-3-(cyclopropylmethoxy)-2H-pyrazolo[4,3-c]quinoline
   Show/Hide
C20H16ClN3O
  1
1
IC50 = 74 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
   Show/Hide
C20H20ClN3O
  1
1
IC50 = 94 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
   Show/Hide
C23H18ClN5O
  1
1
IC50 = 134 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
   Show/Hide
C23H19Cl2N3O
  1
1
IC50 = 157 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
   Show/Hide
C24H21Cl2N3O
  1
1
IC50 = 242 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
   Show/Hide
C22H17Cl2N3O
  1
1
IC50 > 3000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0000163
 Compound Info 
Ambien
   Show/Hide
C19H21N3O
  2
1 EC50 = 198 nM
2 Ki = 20 nM
CP0806010
 Compound Info 
2-(4-chlorophenyl)-2H-pyrazolo[4,3-c]quinolin-3(5H)-one
   Show/Hide
C16H10ClN3O
  1
1 Kd = 0.3 nM
CP0000068
 Compound Info 
Anexate
   Show/Hide
C15H14FN3O3
  2
1 Kd = 2 nM
2 Ki = 0.7943 nM
Clinical Information about the Protein
Target 1 ( GABA(A) receptor alpha-1 (GABRA1) )
Target Type Successful Target
Disease 14 Target-related Diseases  14
1 Postpartum depression [ICD-11: 6E20.0]
2 Insomnia [ICD-11: 7A00-7A0Z]
3 Depression [ICD-11: 6A70-6A7Z]
4 Anxiety disorder [ICD-11: 6B00-6B0Z]
5 Cystitis [ICD-11: GC00]
6 Anaesthesia [ICD-11: 9A78.6]
7 Malaria [ICD-11: 1F40-1F45]
8 Epilepsy [ICD-11: 8A60-8A68]
9 Intractable insomnia [ICD-11: 7A00]
10 Muscle spasm [ICD-11: MB47.3]
11 Epileptic seizures [ICD-11: 8A61-8A6Z]
12 Inflammatory bowel disease [ICD-11: DD72]
13 Premenstrual syndrome [ICD-11: GA34.40]
14 Inflammation [ICD-11: 1A00-CA43.1]
Approved Drug(s) 17 Approved Drugs  17
1 Allopregnanolone
 Drug Info 
Approved
Postpartum depression
2 Amobarbital
 Drug Info 
Approved
Insomnia
3 Barbiturate
 Drug Info 
Approved
Depression
4 Clobazam - Lundbeck
 Drug Info 
Approved
Anxiety disorder
5 Ethanol
 Drug Info 
Approved
Cystitis
6 Hexobarbital
 Drug Info 
Approved
Anaesthesia
7 Indiplon
 Drug Info 
Approved
Insomnia
8 Meprobamate
 Drug Info 
Approved
Malaria
9 Methoxyflurane
 Drug Info 
Approved
Anaesthesia
10 Methylphenobarbital
 Drug Info 
Approved
Anxiety disorder
11 Nitrazepam
 Drug Info 
Approved
Epilepsy
12 Pentobarbital
 Drug Info 
Approved
Insomnia
13 Primidone
 Drug Info 
Approved
Epilepsy
14 Secobarbital
 Drug Info 
Approved
Intractable insomnia
15 THIOCOLCHICOSIDE
 Drug Info 
Approved
Muscle spasm
16 Zaleplon
 Drug Info 
Approved
Insomnia
17 Zolpidem
 Drug Info 
Approved
Insomnia
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 ZK-93423
 Drug Info 
Phase 3
Epileptic seizures
2 GSK683699
 Drug Info 
Phase 2
Inflammatory bowel disease
Discontinued Drug(s) 2 Discontinued Drugs  2
1 ELTANOLONE
 Drug Info 
Discontinued in Phase 3
Premenstrual syndrome
2 U-78875
 Drug Info 
Discontinued in Phase 1
Anxiety disorder
Investigative Drug(s) 1 Investigative Drug  1
1 [3H]CGS8216
 Drug Info 
Investigative
Inflammation