Target Information
| Target General Information | Top | |||||
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| Target ID |
T08910
(Former ID: TTDS00428)
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| Target Name |
GABA(A) receptor gamma-2 (GABRG2)
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| Synonyms |
Gamma-aminobutyric acid receptor subunit gamma-2; GABA(A) receptor subunit gamma-2
Click to Show/Hide
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| Gene Name |
GABRG2
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 3 Target-related Diseases | + | ||||
| 1 | Depression [ICD-11: 6A70-6A7Z] | |||||
| 2 | Mental/behavioural/neurodevelopmental disorder [ICD-11: 6E20-6E8Z] | |||||
| 3 | Tonus and reflex abnormality [ICD-11: MB47] | |||||
| 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.
Click to Show/Hide
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| BioChemical Class |
Neurotransmitter receptor
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| UniProt ID | ||||||
| Sequence |
MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T37CD6 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Allopregnanolone | Drug Info | Approved | Postpartum depression | [2], [3] | |
| 2 | THIOCOLCHICOSIDE | Drug Info | Approved | Muscle spasm | [4] | |
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | ZK-93423 | Drug Info | Phase 3 | Epileptic seizures | [5], [6] | |
| 2 | GSK683699 | Drug Info | Phase 2 | Inflammatory bowel disease | [7] | |
| Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
| 1 | ELTANOLONE | Drug Info | Discontinued in Phase 3 | Premenstrual syndrome | [8] | |
| 2 | U-78875 | Drug Info | Discontinued in Phase 1 | Anxiety disorder | [9] | |
| 3 | CGS-17867A | Drug Info | Terminated | Alcohol dependence | [10] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 116 Inhibitor drugs | + | ||||
| 1 | Allopregnanolone | Drug Info | [11] | |||
| 2 | THIOCOLCHICOSIDE | Drug Info | [1] | |||
| 3 | ZK-93423 | Drug Info | [12] | |||
| 4 | GSK683699 | Drug Info | [1] | |||
| 5 | ELTANOLONE | Drug Info | [11] | |||
| 6 | U-78875 | Drug Info | [13] | |||
| 7 | CGS-17867A | Drug Info | [14] | |||
| 8 | CGS-9896 | Drug Info | [15] | |||
| 9 | (2E,4S)-4-ammoniopent-2-enoate | Drug Info | [16] | |||
| 10 | (4R)-4-ammoniopentanoate | Drug Info | [16] | |||
| 11 | (4S)-4-ammoniopentanoate | Drug Info | [16] | |||
| 12 | (9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine | Drug Info | [17] | |||
| 13 | (beta-CCE)9H-beta-Carboline-3-carboxylic acid | Drug Info | [18] | |||
| 14 | 1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one | Drug Info | [19] | |||
| 15 | 1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one | Drug Info | [20] | |||
| 16 | 1-(4-chlorophenyl)-4-phenyl-1H-imidazole | Drug Info | [15] | |||
| 17 | 1-Methyl-5-oxa-spiro[2.4]heptan-4-one | Drug Info | [19] | |||
| 18 | 2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide | Drug Info | [18] | |||
| 19 | 2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one | Drug Info | [15] | |||
| 20 | 2-(9-Benzyl-9H-purin-6-ylamino)-ethanol | Drug Info | [17] | |||
| 21 | 2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline | Drug Info | [21] | |||
| 22 | 2-Oxa-spiro[4.4]nonan-1-one | Drug Info | [19] | |||
| 23 | 2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline | Drug Info | [21] | |||
| 24 | 3,3-Diethyl-dihydro-furan-2-one | Drug Info | [19] | |||
| 25 | 3,3-Diisopropyl-dihydro-furan-2-one | Drug Info | [19] | |||
| 26 | 3-(3-Methyl-butoxy)-9H-beta-carboline | Drug Info | [22] | |||
| 27 | 3-(benzyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [22] | |||
| 28 | 3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [22] | |||
| 29 | 3-amino-3-demethoxythiocolchicine | Drug Info | [1] | |||
| 30 | 3-Butoxy-9H-beta-carboline | Drug Info | [22] | |||
| 31 | 3-butoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 32 | 3-butoxycarbonyl-6-ethyl-4-quinolone | Drug Info | [23] | |||
| 33 | 3-butylaminocarbonyl-6-ethyl-4-quinolone | Drug Info | [23] | |||
| 34 | 3-carboxy-6-ethyl-4-quinolone | Drug Info | [23] | |||
| 35 | 3-cyclopentoxycarbonyl-6-ethyl-4-quinolone | Drug Info | [23] | |||
| 36 | 3-demethoxy-3-D-lyxopyranosylaminothiocolchicine | Drug Info | [1] | |||
| 37 | 3-demethoxy-3-D-mannopyranosylaminothiocolchicine | Drug Info | [1] | |||
| 38 | 3-demethoxy-3-D-xylopyranosylaminothiocolchicine | Drug Info | [1] | |||
| 39 | 3-demethoxy-3-L-fucopyranosylaminothiocolchicine | Drug Info | [1] | |||
| 40 | 3-demethoxy-3D-glucopyranosylaminothiocolchicine | Drug Info | [1] | |||
| 41 | 3-Ethoxy-9H-beta-carboline | Drug Info | [22], [24] | |||
| 42 | 3-ethoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 43 | 3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone | Drug Info | [23] | |||
| 44 | 3-ethoxycarbonyl-6-propyl-4-quinolone | Drug Info | [23] | |||
| 45 | 3-Ethyl-3-isopropyl-dihydro-furan-2-one | Drug Info | [19] | |||
| 46 | 3-Ethyl-3-methyl-dihydro-furan-2-one | Drug Info | [19] | |||
| 47 | 3-Isobutoxy-9H-beta-carboline | Drug Info | [22] | |||
| 48 | 3-Isopropyl-3-methyl-dihydro-furan-2-one | Drug Info | [19] | |||
| 49 | 3-Isothiocyanato-9H-beta-carboline | Drug Info | [25] | |||
| 50 | 3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one | Drug Info | [20] | |||
| 51 | 3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one | Drug Info | [20] | |||
| 52 | 3-Methyl-9H-beta-carboline | Drug Info | [26] | |||
| 53 | 3-Propoxy-9H-beta-carboline | Drug Info | [22] | |||
| 54 | 3-tert-Butyl-3-ethyl-dihydro-furan-2-one | Drug Info | [19] | |||
| 55 | 4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol | Drug Info | [27] | |||
| 56 | 4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole | Drug Info | [15] | |||
| 57 | 4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol | Drug Info | [28] | |||
| 58 | 4-benzyl-5-(4-piperidyl)isothiazol-3-ol | Drug Info | [29] | |||
| 59 | 4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [30] | |||
| 60 | 4-Methyl-5-(4-piperidyl)isothiazol-3-ol | Drug Info | [29] | |||
| 61 | 4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [30] | |||
| 62 | 4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [30] | |||
| 63 | 4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol | Drug Info | [30] | |||
| 64 | 5-(4-piperidyl)-4-propylisothiazol-3-ol | Drug Info | [29] | |||
| 65 | 5-(piperidin-4-yl)isothiazol-3-ol | Drug Info | [29] | |||
| 66 | 5-(piperidin-4-yl)isoxazol-3-ol | Drug Info | [30] | |||
| 67 | 5-[(1R)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [16] | |||
| 68 | 5-[(1S)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [16] | |||
| 69 | 6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one | Drug Info | [19] | |||
| 70 | 6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one | Drug Info | [19] | |||
| 71 | 6-benzyl-3-ethoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 72 | 6-benzyl-3-propoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 73 | 6-benzyl-3-propylaminocarbonyl-4-quinolone | Drug Info | [23] | |||
| 74 | 6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone | Drug Info | [23] | |||
| 75 | 6-bromo-3-ethoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 76 | 6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone | Drug Info | [23] | |||
| 77 | 6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone | Drug Info | [23] | |||
| 78 | 6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone | Drug Info | [23] | |||
| 79 | 6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone | Drug Info | [23] | |||
| 80 | 6-ethyl-3-i-propoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 81 | 6-ethyl-3-pentoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 82 | 6-ethyl-3-propoxycarbonyl-4-quinolone | Drug Info | [23] | |||
| 83 | 6-ethyl-3-propylaminocarbonyl-4-quinolone | Drug Info | [23] | |||
| 84 | 6-Methyl-2-oxa-spiro[4.4]nonan-1-one | Drug Info | [19] | |||
| 85 | 6-Nitro-2-(3-nitro-phenyl)-chromen-4-one | Drug Info | [31] | |||
| 86 | 6-Nitro-2-(4-nitro-phenyl)-chromen-4-one | Drug Info | [31] | |||
| 87 | 9H-beta-Carboline-3-carboxylic acid ethyl ester | Drug Info | [22], [32] | |||
| 88 | 9H-beta-Carboline-3-carboxylic acid propyl ester | Drug Info | [32] | |||
| 89 | AMENTOFLAVONE | Drug Info | [33] | |||
| 90 | Beta-Carboline-3-carboxylic acid t-butyl ester | Drug Info | [22] | |||
| 91 | BETA-CCM | Drug Info | [32] | |||
| 92 | CGS-13767 | Drug Info | [34] | |||
| 93 | CGS-9895 | Drug Info | [35] | |||
| 94 | CI-218872 | Drug Info | [26] | |||
| 95 | Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [22] | |||
| 96 | GNF-PF-3645 | Drug Info | [23] | |||
| 97 | GNF-PF-4421 | Drug Info | [23] | |||
| 98 | L-655708 | Drug Info | [36] | |||
| 99 | N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide | Drug Info | [37] | |||
| 100 | N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide | Drug Info | [37] | |||
| 101 | N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide | Drug Info | [37] | |||
| 102 | N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide | Drug Info | [37] | |||
| 103 | N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide | Drug Info | [37] | |||
| 104 | N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide | Drug Info | [38] | |||
| 105 | Ridine-5-carboxylic acid ethyl ester | Drug Info | [39] | |||
| 106 | RO-145974 | Drug Info | [40] | |||
| 107 | RO-145975 | Drug Info | [40] | |||
| 108 | RO-147437 | Drug Info | [40] | |||
| 109 | Ro-15-3505 | Drug Info | [40] | |||
| 110 | RO-194603 | Drug Info | [40] | |||
| 111 | Ro-4938581 | Drug Info | [41] | |||
| 112 | RY-066 | Drug Info | [42] | |||
| 113 | Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [22] | |||
| 114 | U-89267 | Drug Info | [44] | |||
| 115 | [3H]CGS8216 | Drug Info | [34] | |||
| 116 | [3H]Ro154513 | Drug Info | [44] | |||
| Blocker (channel blocker) | [+] 1 Blocker (channel blocker) drugs | + | ||||
| 1 | TBPS | Drug Info | [43] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Diazepam | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus diazepam | PDB:6X3X | ||||
| Method | Electron microscopy | Resolution | 2.92 Å | Mutation | No | [45] |
| PDB Sequence |
GDVTVILNNL
34 LEGYDNKLRP44 DIGVKPTLIH54 TDMYVNSIGP64 VNAINMEYTI74 DIFFAQTWYD 84 RRLKFNSTIK94 VLRLNSNMVG104 KIWIPDTFFR114 NSKKADAHWI124 TTPNRMLRIW 134 NDGRVLYTLR144 LTIDAECQLQ154 LHNFPMDEHS164 CPLEFSSYGY174 PREEIVYQWK 184 RSSVEVGDTR194 SWRLYQFSFV204 GLRNTTEVVK214 TTSGDYVVMS224 VYFDLSRRMG 234 YFTIQTYIPC244 TLIVVLSWVS254 FWINKDAVPA264 RTSLGITTVL274 TMTTLSTIAR 284 KSLPKVSYVT294 AMDLFVSVCF304 IFVFSALVEY314 GTLHYFVSSQ324 PARAAKMDSY 334 ARIFFPTAFC344 LFNLVYWVSY354 LYL
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| Ligand Name: Phenobarbital | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus phenobarbital | PDB:6X3W | ||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | No | [45] |
| PDB Sequence |
GDVTVILNNL
34 LEGYDNKLRP44 DIGVKPTLIH54 TDMYVNSIGP64 VNAINMEYTI74 DIFFAQTWYD 84 RRLKFNSTIK94 VLRLNSNMVG104 KIWIPDTFFR114 NSKKADAHWI124 TTPNRMLRIW 134 NDGRVLYTLR144 LTIDAECQLQ154 LHNFPMDEHS164 CPLEFSSYGY174 PREEIVYQWK 184 RSSVEVGDTR194 SWRLYQFSFV204 GLRNTTEVVK214 TTSGDYVVMS224 VYFDLSRRMG 234 YFTIQTYIPC244 TLIVVLSWVS254 FWINKDAVPA264 RTSLGITTVL274 TMTTLSTIAR 284 KSLPKVSYVT294 AMDLFVSVCF304 IFVFSALVEY314 GTLHYFVSSQ324 PARAAKMDSY 334 ARIFFPTAFC344 LFNLVYWVSY354 LYL
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Retrograde endocannabinoid signaling | hsa04723 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| GABAergic synapse | hsa04727 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 1.45E-01 | Radiality | 1.18E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 5.00E+00 | Topological coefficient | 1.00E+00 | Eccentricity | 14 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 5 KEGG Pathways | + | ||||
| 1 | Neuroactive ligand-receptor interaction | |||||
| 2 | Retrograde endocannabinoid signaling | |||||
| 3 | GABAergic synapse | |||||
| 4 | Morphine addiction | |||||
| 5 | Nicotine addiction | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Ligand-gated ion channel transport | |||||
| 2 | GABA A receptor activation | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | |||||
| 2 | Iron uptake and transport | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7. | |||||
| REF 2 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4346). | |||||
| REF 6 | Abecarnil enhances GABA-induced currents in acutely isolated cerebellar Purkinje cells. Neuropharmacology. 1995 Feb;34(2):157-63. | |||||
| REF 7 | Emerging drugs to treat Crohn's disease. Expert Opin Emerg Drugs. 2007 Mar;12(1):49-59. | |||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005875) | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001194) | |||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000696) | |||||
| REF 11 | Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (... J Med Chem. 2005 Apr 21;48(8):3051-9. | |||||
| REF 12 | Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9. | |||||
| REF 13 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepin... J Med Chem. 1996 Sep 13;39(19):3820-36. | |||||
| REF 14 | 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4. | |||||
| REF 15 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. J Med Chem. 2006 Mar 23;49(6):1855-66. | |||||
| REF 16 | gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83. | |||||
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