Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT06RH5)

• DTT Name: GABA(A) receptor gamma-2 (GABRG2)
• Synonyms: Gamma-aminobutyric acid receptor subunit gamma-2; GABA(A) receptor subunit gamma-2
• Gene Name: GABRG2
• DTT Type: Successful target; [1]
• BioChemical Class: Neurotransmitter receptor
• UniProt ID: GBRG2_HUMAN
• TTD ID: T08910
• Sequence:
  MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
  VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
  WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
  TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
  SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
  VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
  SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
  FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
• Function: Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel. 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. The alpha1/beta2/gamma2 receptor and the alpha1/beta3/gamma2 receptor exhibit synaptogenic activity. The alpha2/beta2/gamma2 receptor exhibits synatogenic activity whereas the alpha2/beta3/gamma2 receptor shows very little or no synaptogenic activity. Functions also as histamine receptor and mediates cellular responses to histamine. Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Retrograde endocannabinoid signaling (hsa04723)
  GABAergic synapse (hsa04727)
  Morphine addiction (hsa05032)
  Nicotine addiction (hsa05033)
• Reactome Pathway:
  GABA A receptor activation (R-HSA-977441)
  Ligand-gated ion channel transport (R-HSA-975298)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[2]
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[1]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ZK-93423	DMFWMKZ	Epileptic seizures	8A61-8A6Z	Phase 3	[3]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[1]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ELTANOLONE	DM38CIV	Premenstrual syndrome	GA34.40	Discontinued in Phase 3	[2]
U-78875	DM2WOPX	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[4]
CGS-17867A	DMMZJY3	Alcohol dependence	6C40.2	Terminated	[5]
CGS-9896	DM39PQI	N. A.	N. A.	Terminated	[6]

109 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(2E,4S)-4-ammoniopent-2-enoate	DMA9RIS	Discovery agent	N.A.	Investigative	[7]
(4R)-4-ammoniopentanoate	DMZFTI4	Discovery agent	N.A.	Investigative	[7]
(4S)-4-ammoniopentanoate	DMBLAY1	Discovery agent	N.A.	Investigative	[7]
(9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine	DMHJG5N	Discovery agent	N.A.	Investigative	[8]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid	DMVWQ26	Discovery agent	N.A.	Investigative	[9]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one	DMOGHRS	Discovery agent	N.A.	Investigative	[10]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one	DM1KND6	Discovery agent	N.A.	Investigative	[11]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole	DMVCHSI	Discovery agent	N.A.	Investigative	[6]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one	DMX2FWN	Discovery agent	N.A.	Investigative	[10]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide	DMFAME4	Discovery agent	N.A.	Investigative	[9]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one	DMYGRS9	Discovery agent	N.A.	Investigative	[6]
2-(9-Benzyl-9H-purin-6-ylamino)-ethanol	DMPJ0O6	Discovery agent	N.A.	Investigative	[8]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline	DMD2ZNA	Discovery agent	N.A.	Investigative	[12]
2-Oxa-spiro[4.4]nonan-1-one	DM2NEX4	Discovery agent	N.A.	Investigative	[10]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline	DMPF598	Discovery agent	N.A.	Investigative	[12]
3,3-Diethyl-dihydro-furan-2-one	DMFJ9N0	Discovery agent	N.A.	Investigative	[10]
3,3-Diisopropyl-dihydro-furan-2-one	DMIFUDG	Discovery agent	N.A.	Investigative	[10]
3-(3-Methyl-butoxy)-9H-beta-carboline	DMTNCXP	Discovery agent	N.A.	Investigative	[13]
3-(benzyloxy)-9H-pyrido[3,4-b]indole	DMDNEKR	Discovery agent	N.A.	Investigative	[13]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole	DMKHNTY	Discovery agent	N.A.	Investigative	[13]
3-amino-3-demethoxythiocolchicine	DM60K7H	Discovery agent	N.A.	Investigative	[1]
3-Butoxy-9H-beta-carboline	DMQ8H74	Discovery agent	N.A.	Investigative	[13]
3-butoxycarbonyl-4-quinolone	DMRF2Q8	Discovery agent	N.A.	Investigative	[14]
3-butoxycarbonyl-6-ethyl-4-quinolone	DMD6PMZ	Discovery agent	N.A.	Investigative	[14]
3-butylaminocarbonyl-6-ethyl-4-quinolone	DM95XWR	Discovery agent	N.A.	Investigative	[14]
3-carboxy-6-ethyl-4-quinolone	DMRUX93	Discovery agent	N.A.	Investigative	[14]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone	DMEL8S5	Discovery agent	N.A.	Investigative	[14]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine	DME8VPC	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine	DMALMGH	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine	DMXFVD1	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine	DM4ERYF	Discovery agent	N.A.	Investigative	[1]
3-demethoxy-3D-glucopyranosylaminothiocolchicine	DMID7TC	Discovery agent	N.A.	Investigative	[1]
3-Ethoxy-9H-beta-carboline	DM6K7BI	Discovery agent	N.A.	Investigative	[15]
3-ethoxycarbonyl-4-quinolone	DMY4VOI	Discovery agent	N.A.	Investigative	[14]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone	DMMDOI4	Discovery agent	N.A.	Investigative	[14]
3-ethoxycarbonyl-6-propyl-4-quinolone	DM1E5QZ	Discovery agent	N.A.	Investigative	[14]
3-Ethyl-3-isopropyl-dihydro-furan-2-one	DMZK13I	Discovery agent	N.A.	Investigative	[10]
3-Ethyl-3-methyl-dihydro-furan-2-one	DM1VTFU	Discovery agent	N.A.	Investigative	[10]
3-Isobutoxy-9H-beta-carboline	DM6X5TZ	Discovery agent	N.A.	Investigative	[13]
3-Isopropyl-3-methyl-dihydro-furan-2-one	DMSLPGZ	Discovery agent	N.A.	Investigative	[10]
3-Isothiocyanato-9H-beta-carboline	DM9LEWH	Discovery agent	N.A.	Investigative	[16]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one	DMTM6B0	Discovery agent	N.A.	Investigative	[11]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one	DM870UV	Discovery agent	N.A.	Investigative	[11]
3-Methyl-9H-beta-carboline	DMEJKZN	Discovery agent	N.A.	Investigative	[17]
3-Propoxy-9H-beta-carboline	DMDEV64	Discovery agent	N.A.	Investigative	[13]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one	DMGDT8V	Discovery agent	N.A.	Investigative	[10]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol	DMCS538	Discovery agent	N.A.	Investigative	[18]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole	DMJI6QH	Discovery agent	N.A.	Investigative	[6]
4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol	DM1T95Y	Discovery agent	N.A.	Investigative	[19]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol	DMZ18OJ	Discovery agent	N.A.	Investigative	[20]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol	DMA4CZK	Discovery agent	N.A.	Investigative	[21]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol	DMV19HC	Discovery agent	N.A.	Investigative	[20]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol	DMEIA3L	Discovery agent	N.A.	Investigative	[21]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol	DM9O8UM	Discovery agent	N.A.	Investigative	[21]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol	DM7E4JU	Discovery agent	N.A.	Investigative	[21]
5-(4-piperidyl)-4-propylisothiazol-3-ol	DMZ7K5G	Discovery agent	N.A.	Investigative	[20]
5-(piperidin-4-yl)isothiazol-3-ol	DM4XGFW	Discovery agent	N.A.	Investigative	[20]
5-(piperidin-4-yl)isoxazol-3-ol	DM6GO2I	Discovery agent	N.A.	Investigative	[21]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate	DM23PL4	Discovery agent	N.A.	Investigative	[7]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate	DMYAPLT	Discovery agent	N.A.	Investigative	[7]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one	DMOIFAP	Discovery agent	N.A.	Investigative	[10]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one	DM7FMWS	Discovery agent	N.A.	Investigative	[10]
6-benzyl-3-ethoxycarbonyl-4-quinolone	DMICRFQ	Discovery agent	N.A.	Investigative	[14]
6-benzyl-3-propoxycarbonyl-4-quinolone	DMXMI5E	Discovery agent	N.A.	Investigative	[14]
6-benzyl-3-propylaminocarbonyl-4-quinolone	DM7HNPJ	Discovery agent	N.A.	Investigative	[14]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone	DM4HRIX	Discovery agent	N.A.	Investigative	[14]
6-bromo-3-ethoxycarbonyl-4-quinolone	DM0MQHP	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone	DMLEUP2	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone	DMESU53	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone	DM1POEA	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone	DMG05V1	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-i-propoxycarbonyl-4-quinolone	DML9EU7	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-pentoxycarbonyl-4-quinolone	DMSGJM6	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-propoxycarbonyl-4-quinolone	DMGVI08	Discovery agent	N.A.	Investigative	[14]
6-ethyl-3-propylaminocarbonyl-4-quinolone	DMC1F2E	Discovery agent	N.A.	Investigative	[14]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one	DMNJRFP	Discovery agent	N.A.	Investigative	[10]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one	DMRCTBA	Discovery agent	N.A.	Investigative	[22]
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one	DMM635K	Discovery agent	N.A.	Investigative	[22]
9H-beta-Carboline-3-carboxylic acid ethyl ester	DMK459I	Discovery agent	N.A.	Investigative	[13]
9H-beta-Carboline-3-carboxylic acid propyl ester	DMMUH98	Discovery agent	N.A.	Investigative	[23]
AMENTOFLAVONE	DMLRNV2	Discovery agent	N.A.	Investigative	[24]
Beta-Carboline-3-carboxylic acid t-butyl ester	DM9LT60	N. A.	N. A.	Investigative	[13]
BETA-CCM	DM1MFTZ	Discovery agent	N.A.	Investigative	[23]
CGS-13767	DM4DSE7	Discovery agent	N.A.	Investigative	[25]
CGS-9895	DMKY6CU	Discovery agent	N.A.	Investigative	[26]
CI-218872	DM0RH3S	Discovery agent	N.A.	Investigative	[17]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate	DM5G91Z	Discovery agent	N.A.	Investigative	[13]
GNF-PF-3645	DM17GIV	Discovery agent	N.A.	Investigative	[14]
GNF-PF-4421	DMV10UH	Discovery agent	N.A.	Investigative	[14]
L-655708	DM4CDIB	Discovery agent	N.A.	Investigative	[27]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide	DMULBO9	Discovery agent	N.A.	Investigative	[28]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide	DM8A23B	Discovery agent	N.A.	Investigative	[28]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide	DMMT65J	Discovery agent	N.A.	Investigative	[28]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide	DM157LQ	Discovery agent	N.A.	Investigative	[28]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide	DMH7Z4L	Discovery agent	N.A.	Investigative	[28]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide	DM8ZMB5	Discovery agent	N.A.	Investigative	[29]
Ridine-5-carboxylic acid ethyl ester	DM9HMCS	Discovery agent	N.A.	Investigative	[30]
RO-145974	DM0ACKJ	Discovery agent	N.A.	Investigative	[31]
RO-145975	DMAJ6BW	Discovery agent	N.A.	Investigative	[31]
RO-147437	DMX4B36	Discovery agent	N.A.	Investigative	[31]
Ro-15-3505	DM4NW3U	Discovery agent	N.A.	Investigative	[31]
RO-194603	DM8C2Z0	Discovery agent	N.A.	Investigative	[31]
Ro-4938581	DMCB2N9	Discovery agent	N.A.	Investigative	[32]
RY-066	DMGUX16	Discovery agent	N.A.	Investigative	[33]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate	DM9QSDC	Discovery agent	N.A.	Investigative	[13]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[34]
U-89267	DMQT6AH	Discovery agent	N.A.	Investigative	[35]
[3H]CGS8216	DMLP68J	Inflammation	1A00-CA43.1	Investigative	[25]
[3H]Ro154513	DMMBWKL	Discovery agent	N.A.	Investigative	[35]

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