Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTZA1NY)

• DTT Name: GABA(A) receptor beta-2 (GABRB2)
• Synonyms: GABRB2; GABA(A) receptor subunit beta-2
• Gene Name: GABRB2
• DTT Type: Successful target; [1]
• BioChemical Class: Neurotransmitter receptor
• UniProt ID: GBRB2_HUMAN
• TTD ID: T80387
• Sequence:
  MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
  AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
  YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
  YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
  NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
  YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKI
  FYKDIKQNGTQYRSLWDPTGNLSPTRRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEA
  VMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPD
  LTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
• Function: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand- gated chloride channel.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Retrograde endocannabinoid signaling (hsa04723)
  Serotonergic synapse (hsa04726)
  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

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[2]
Ethchlorvynol	DM53IP1	Insomnia	7A00-7A0Z	Approved	[1]
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[3]

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	[4]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[3]

3 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	[5]
CGS-9896	DM39PQI	N. A.	N. A.	Terminated	[6]

82 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]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one	DMOGHRS	Discovery agent	N.A.	Investigative	[9]
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	[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	[10]
2-Oxa-spiro[4.4]nonan-1-one	DM2NEX4	Discovery agent	N.A.	Investigative	[9]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline	DMPF598	Discovery agent	N.A.	Investigative	[10]
3,3-Diethyl-dihydro-furan-2-one	DMFJ9N0	Discovery agent	N.A.	Investigative	[9]
3,3-Diisopropyl-dihydro-furan-2-one	DMIFUDG	Discovery agent	N.A.	Investigative	[9]
3-amino-3-demethoxythiocolchicine	DM60K7H	Discovery agent	N.A.	Investigative	[3]
3-butoxycarbonyl-4-quinolone	DMRF2Q8	Discovery agent	N.A.	Investigative	[11]
3-butoxycarbonyl-6-ethyl-4-quinolone	DMD6PMZ	Discovery agent	N.A.	Investigative	[11]
3-butylaminocarbonyl-6-ethyl-4-quinolone	DM95XWR	Discovery agent	N.A.	Investigative	[11]
3-carboxy-6-ethyl-4-quinolone	DMRUX93	Discovery agent	N.A.	Investigative	[11]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone	DMEL8S5	Discovery agent	N.A.	Investigative	[11]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine	DME8VPC	Discovery agent	N.A.	Investigative	[3]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine	DMALMGH	Discovery agent	N.A.	Investigative	[3]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine	DMXFVD1	Discovery agent	N.A.	Investigative	[3]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine	DM4ERYF	Discovery agent	N.A.	Investigative	[3]
3-demethoxy-3D-glucopyranosylaminothiocolchicine	DMID7TC	Discovery agent	N.A.	Investigative	[3]
3-ethoxycarbonyl-4-quinolone	DMY4VOI	Discovery agent	N.A.	Investigative	[11]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone	DMMDOI4	Discovery agent	N.A.	Investigative	[11]
3-ethoxycarbonyl-6-propyl-4-quinolone	DM1E5QZ	Discovery agent	N.A.	Investigative	[11]
3-Ethyl-3-isopropyl-dihydro-furan-2-one	DMZK13I	Discovery agent	N.A.	Investigative	[9]
3-Ethyl-3-methyl-dihydro-furan-2-one	DM1VTFU	Discovery agent	N.A.	Investigative	[9]
3-Isopropyl-3-methyl-dihydro-furan-2-one	DMSLPGZ	Discovery agent	N.A.	Investigative	[9]
3-Isothiocyanato-9H-beta-carboline	DM9LEWH	Discovery agent	N.A.	Investigative	[12]
3-Methyl-9H-beta-carboline	DMEJKZN	Discovery agent	N.A.	Investigative	[13]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one	DMGDT8V	Discovery agent	N.A.	Investigative	[9]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol	DMCS538	Discovery agent	N.A.	Investigative	[14]
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	[15]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol	DMA4CZK	Discovery agent	N.A.	Investigative	[16]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol	DMEIA3L	Discovery agent	N.A.	Investigative	[16]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol	DM9O8UM	Discovery agent	N.A.	Investigative	[16]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol	DM7E4JU	Discovery agent	N.A.	Investigative	[16]
5-(piperidin-4-yl)isoxazol-3-ol	DM6GO2I	Discovery agent	N.A.	Investigative	[16]
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	[9]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one	DM7FMWS	Discovery agent	N.A.	Investigative	[9]
6-benzyl-3-ethoxycarbonyl-4-quinolone	DMICRFQ	Discovery agent	N.A.	Investigative	[11]
6-benzyl-3-propoxycarbonyl-4-quinolone	DMXMI5E	Discovery agent	N.A.	Investigative	[11]
6-benzyl-3-propylaminocarbonyl-4-quinolone	DM7HNPJ	Discovery agent	N.A.	Investigative	[11]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone	DM4HRIX	Discovery agent	N.A.	Investigative	[11]
6-bromo-3-ethoxycarbonyl-4-quinolone	DM0MQHP	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone	DMLEUP2	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone	DMESU53	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone	DM1POEA	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone	DMG05V1	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-i-propoxycarbonyl-4-quinolone	DML9EU7	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-pentoxycarbonyl-4-quinolone	DMSGJM6	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-propoxycarbonyl-4-quinolone	DMGVI08	Discovery agent	N.A.	Investigative	[11]
6-ethyl-3-propylaminocarbonyl-4-quinolone	DMC1F2E	Discovery agent	N.A.	Investigative	[11]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one	DMNJRFP	Discovery agent	N.A.	Investigative	[9]
AMENTOFLAVONE	DMLRNV2	Discovery agent	N.A.	Investigative	[17]
BETA-CCM	DM1MFTZ	Discovery agent	N.A.	Investigative	[13]
CGS-13767	DM4DSE7	Discovery agent	N.A.	Investigative	[18]
CI-218872	DM0RH3S	Discovery agent	N.A.	Investigative	[13]
GNF-PF-3645	DM17GIV	Discovery agent	N.A.	Investigative	[11]
GNF-PF-4421	DMV10UH	Discovery agent	N.A.	Investigative	[11]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide	DMULBO9	Discovery agent	N.A.	Investigative	[19]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide	DM8A23B	Discovery agent	N.A.	Investigative	[19]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide	DMMT65J	Discovery agent	N.A.	Investigative	[19]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide	DM157LQ	Discovery agent	N.A.	Investigative	[19]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide	DMH7Z4L	Discovery agent	N.A.	Investigative	[19]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide	DM8ZMB5	Discovery agent	N.A.	Investigative	[20]
Ridine-5-carboxylic acid ethyl ester	DM9HMCS	Discovery agent	N.A.	Investigative	[21]
RO-145974	DM0ACKJ	Discovery agent	N.A.	Investigative	[22]
RO-145975	DMAJ6BW	Discovery agent	N.A.	Investigative	[22]
RO-147437	DMX4B36	Discovery agent	N.A.	Investigative	[22]
Ro-15-3505	DM4NW3U	Discovery agent	N.A.	Investigative	[22]
RO-194603	DM8C2Z0	Discovery agent	N.A.	Investigative	[22]
TBPS	DMFC3XP	Discovery agent	N.A.	Investigative	[23]
U-89267	DMQT6AH	Discovery agent	N.A.	Investigative	[24]
[3H]CGS8216	DMLP68J	Inflammation	1A00-CA43.1	Investigative	[25]
[3H]Ro154513	DMMBWKL	Discovery agent	N.A.	Investigative	[22]

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