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Target Report Card

Target Name and Classification

Target ID CHEMBL2093872
Target Type PROTEIN COMPLEX GROUP
Preferred Name GABA-A receptor; anion channel
Synonyms GABA(A) receptor subunit alpha-1 | GABA(A) receptor subunit alpha-2 | GABA(A) receptor subunit alpha-3 | GABA(A) receptor subunit alpha-4 | GABA(A) receptor subunit alpha-5 | GABA(A) receptor subunit alpha-6 | GABA(A) receptor subunit beta-1 | GABA(A) receptor subunit beta-2 | GABA(A) receptor subunit beta-3 | GABA(A) receptor subunit delta | GABA(A) receptor subunit epsilon | GABA(A) receptor subunit gamma-1 | GABA(A) receptor subunit gamma-2 | GABA(A) receptor subunit gamma-3 | GABA(A) receptor subunit pi | GABA(A) receptor subunit theta | GABRA1 | GABRA2 | GABRA3 | GABRA4 | GABRA5 | GABRA6 | GABRB1 | GABRB2 | GABRB3 | GABRD | GABRE | GABRG1 | GABRG2 | GABRG3 | GABRP | GABRQ | Gamma-aminobutyric acid receptor subunit alpha-1 | Gamma-aminobutyric acid receptor subunit alpha-2 | Gamma-aminobutyric acid receptor subunit alpha-3 | Gamma-aminobutyric acid receptor subunit alpha-4 | Gamma-aminobutyric acid receptor subunit alpha-5 | Gamma-aminobutyric acid receptor subunit alpha-6 | Gamma-aminobutyric acid receptor subunit beta-1 | Gamma-aminobutyric acid receptor subunit beta-2 | Gamma-aminobutyric acid receptor subunit beta-3 | Gamma-aminobutyric acid receptor subunit delta | Gamma-aminobutyric acid receptor subunit epsilon | Gamma-aminobutyric acid receptor subunit gamma-1 | Gamma-aminobutyric acid receptor subunit gamma-2 | Gamma-aminobutyric acid receptor subunit gamma-3 | Gamma-aminobutyric acid receptor subunit pi | Gamma-aminobutyric acid receptor subunit theta
Organism Homo sapiens
Species Group No
Protein Target Classification
  • ion channel > ligand-gated ion channel > gaba-a receptor

Target Components

Component Description Relationship Accession
Gamma-aminobutyric acid receptor subunit theta GROUP MEMBER Q9UN88
Gamma-aminobutyric acid receptor subunit beta-3 GROUP MEMBER P28472
Gamma-aminobutyric acid receptor subunit alpha-1 GROUP MEMBER P14867
Gamma-aminobutyric acid receptor subunit alpha-4 GROUP MEMBER P48169
Gamma-aminobutyric acid receptor subunit delta GROUP MEMBER O14764
Gamma-aminobutyric acid receptor subunit alpha-5 GROUP MEMBER P31644
Gamma-aminobutyric acid receptor subunit gamma-3 GROUP MEMBER Q99928
Gamma-aminobutyric acid receptor subunit epsilon GROUP MEMBER P78334
Gamma-aminobutyric acid receptor subunit gamma-1 GROUP MEMBER Q8N1C3
Gamma-aminobutyric acid receptor subunit alpha-3 GROUP MEMBER P34903
Gamma-aminobutyric acid receptor subunit pi GROUP MEMBER O00591
Gamma-aminobutyric acid receptor subunit beta-2 GROUP MEMBER P47870
Gamma-aminobutyric acid receptor subunit gamma-2 GROUP MEMBER P18507
Gamma-aminobutyric acid receptor subunit beta-1 GROUP MEMBER P18505
Gamma-aminobutyric acid receptor subunit alpha-6 GROUP MEMBER Q16445
Gamma-aminobutyric acid receptor subunit alpha-2 GROUP MEMBER P47869

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3885577 Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-3 PROTEIN COMPLEX
CHEMBL3885576 Gamma-aminobutyric acid receptor subunit alpha-5/beta-2 PROTEIN COMPLEX
CHEMBL2094122 GABA-A receptor; alpha-5/beta-3/gamma-2 PROTEIN COMPLEX
CHEMBL3885578 Gamma-aminobutyric acid receptor subunit alpha-6/beta-3 PROTEIN COMPLEX
CHEMBL2095190 GABA-A receptor; alpha-6/beta-3/gamma-2 PROTEIN COMPLEX
CHEMBL2579 GABA receptor alpha-6 subunit SINGLE PROTEIN
CHEMBL2109244 GABA-A receptor; agonist GABA site PROTEIN COMPLEX GROUP
CHEMBL2109243 GABA-A receptor; benzodiazepine site PROTEIN COMPLEX GROUP
CHEMBL2094130 GABA-A receptor; alpha-2/beta-3/gamma-2 PROTEIN COMPLEX
CHEMBL1962 GABA receptor alpha-1 subunit SINGLE PROTEIN
CHEMBL2111339 GABA A receptor alpha-3/beta-2/gamma-2 PROTEIN COMPLEX
CHEMBL3591 GABA receptor delta subunit SINGLE PROTEIN
CHEMBL3026 GABA receptor alpha-3 subunit SINGLE PROTEIN
CHEMBL2111413 GABA A receptor alpha-2/beta-2/gamma-2 PROTEIN COMPLEX
CHEMBL1920 GABA receptor beta-2 subunit SINGLE PROTEIN
CHEMBL2111366 GABA A receptor alpha-4/beta-3/gamma-2 PROTEIN COMPLEX
CHEMBL4956 GABA receptor alpha-2 subunit SINGLE PROTEIN
CHEMBL2111370 GABA A receptor alpha-6/beta-2/gamma-2 PROTEIN COMPLEX
CHEMBL1907597 GABA-A receptor; GABA-A site (alpha1/beta2 interface) PROTEIN COMPLEX
CHEMBL1847 GABA receptor beta-3 subunit SINGLE PROTEIN
CHEMBL5112 GABA receptor alpha-5 subunit SINGLE PROTEIN
CHEMBL2095172 GABA-A receptor; alpha-1/beta-2/gamma-2 PROTEIN COMPLEX
CHEMBL2472 GABA receptor alpha-4 subunit SINGLE PROTEIN
CHEMBL3885571 Gamma-aminobutyric acid receptor subunit alpha-2/beta-2 PROTEIN COMPLEX
CHEMBL3885570 Gamma-aminobutyric acid receptor subunit alpha-1/ beta-1 PROTEIN COMPLEX
CHEMBL3885573 Gamma-aminobutyric acid receptor subunit alpha-3/ beta-3/gamma-3 PROTEIN COMPLEX
CHEMBL3885572 Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2 PROTEIN COMPLEX
CHEMBL2111392 GABA A receptor alpha-1/beta-1/gamma-2 PROTEIN COMPLEX
CHEMBL3885575 Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta PROTEIN COMPLEX
CHEMBL2094121 GABA-A receptor; alpha-1/beta-3/gamma-2 PROTEIN COMPLEX
CHEMBL2094120 GABA-A receptor; alpha-3/beta-3/gamma-2 PROTEIN COMPLEX
CHEMBL3885574 Gamma-aminobutyric acid receptor subunit alpha-3/beta-3 PROTEIN COMPLEX

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL407 FLUMAZENIL GABA-A receptor; anion channel allosteric antagonist 4 FDA
CHEMBL12 DIAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL448 PENTOBARBITAL GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL450 METHARBITAL GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL451 CHLORDIAZEPOXIDE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL452 CLONAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL454 BUTALBITAL GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL13280 FLUNITRAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 Other PubMed PubMed PubMed
CHEMBL526 PROPOFOL GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL568 OXAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL580 LORAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL591 ETHCHLORVYNOL GABA-A receptor; anion channel positive modulator 4 ISBN PubMed
CHEMBL282052 METHAQUALONE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL646 TRIAZOLAM GABA-A receptor; anion channel positive allosteric modulator 4 FDA ISBN
CHEMBL661 ALPRAZOLAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL681 ETOMIDATE GABA-A receptor; anion channel positive modulator 4 PubMed PubMed
CHEMBL738 THIOPENTAL SODIUM GABA-A receptor; anion channel positive allosteric modulator 4 ISBN PubMed
CHEMBL30219 METHOHEXITAL SODIUM GABA-A receptor; anion channel positive allosteric modulator 4 ISBN PubMed
CHEMBL285674 ESTAZOLAM GABA-A receptor; anion channel positive allosteric modulator 4 ISBN PubMed
CHEMBL856 PRIMIDONE GABA-A receptor; anion channel positive allosteric modulator 4 ISBN PubMed
CHEMBL931 HALOTHANE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL967 TEMAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 FDA
CHEMBL969 PRAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL970 HALAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL971 PENTOBARBITAL SODIUM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL979 MEPROBAMATE GABA-A receptor; anion channel agonist 4 PubMed
CHEMBL70418 CLOBAZAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL315795 CLOMETHIAZOLE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed PubMed PubMed PubMed PubMed PubMed
CHEMBL1102 GLUTETHIMIDE GABA-A receptor; anion channel positive modulator 4 ISBN PubMed
CHEMBL1256 ISOFLURANE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL1257 ENFLURANE GABA-A receptor; anion channel positive modulator 4 PubMed PubMed PubMed
CHEMBL1341 METHOXYFLURANE GABA-A receptor; anion channel positive modulator 4 PubMed PubMed
CHEMBL220492 TOPIRAMATE GABA-A receptor; anion channel positive modulator 4 DailyMed PubMed
CHEMBL1522 ESZOPICLONE GABA-A receptor; anion channel positive allosteric modulator 4 FDA PubMed
CHEMBL1200420 MIDAZOLAM HYDROCHLORIDE GABA-A receptor; anion channel positive allosteric modulator 4 ISBN
CHEMBL1200472 QUAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL1200694 SEVOFLURANE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed
CHEMBL1200703 CHLORDIAZEPOXIDE HYDROCHLORIDE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL1200733 DESFLURANE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL1200789 TRICLOFOS SODIUM GABA-A receptor; anion channel positive modulator 4 PubMed
CHEMBL1200790 METHYPRYLON GABA-A receptor; anion channel positive allosteric modulator 4 ISBN PubMed
CHEMBL1200802 TALBUTAL GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL1200903 SECOBARBITAL SODIUM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL1200982 BUTABARBITAL SODIUM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL1201065 THIAMYLAL SODIUM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed PubMed
CHEMBL1697737 CLOTIAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL2068724 ACAMPROSATE CALCIUM GABA-A receptor; anion channel positive modulator 4 FDA PubMed
CHEMBL2096631 CLORAZEPATE DIPOTASSIUM GABA-A receptor; anion channel positive allosteric modulator 4 FDA ISBN
CHEMBL2105527 TETRAZEPAM GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed PubMed PubMed PubMed PubMed
CHEMBL2106829 METHAQUALONE HYDROCHLORIDE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed PubMed
CHEMBL3989724 FLURAZEPAM HYDROCHLORIDE GABA-A receptor; anion channel positive allosteric modulator 4 PubMed
CHEMBL1568698 GANAXOLONE GABA-A receptor; anion channel positive allosteric modulator 3 PubMed PubMed PubMed
CHEMBL2103791 ADIPIPLON GABA-A receptor; anion channel partial agonist 2 Other
CHEMBL2104745 PAGOCLONE GABA-A receptor; anion channel positive allosteric modulator 2 PubMed PubMed PubMed
CHEMBL2107801 RESEQUINIL GABA-A receptor; anion channel inverse agonist 2 PubMed
CHEMBL3707402 PF-06372865 GABA-A receptor; anion channel agonist 2 Other Other
CHEMBL3707317 LOREDIPLON GABA-A receptor; anion channel positive allosteric modulator 0 PubMed PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

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