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TargetGABA-A receptor; alpha-5/beta-3/gamma-2
LigandBDBM50143088
Substrate/Competitorn/a
Meas. Tech.ChEMBL_69797 (CHEMBL678745)
Ki 0.5±n/a nM
Citation Carling, RWMoore, KWStreet, LJWild, DIsted, CLeeson, PDThomas, SO'Connor, DMcKernan, RMQuirk, KCook, SMAtack, JRWafford, KAThompson, SADawson, GRFerris, PCastro, JL 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. J Med Chem47:1807-22 (2004) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
GABA-A receptor; alpha-5/beta-3/gamma-2
Name:GABA-A receptor; alpha-5/beta-3/gamma-2
Synonyms:GABA receptor alpha-5/beta-3/gamma-2 subunit | Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 2148177
Components:This complex has 3 components.
Component 1
Name:Gamma-aminobutyric acid receptor subunit gamma-2
Synonyms:GABA(A) receptor subunit gamma-2 | GABRG2 | GBRG2_HUMAN
Type:PROTEIN
Mol. Mass.:54172.74
Organism:Homo sapiens (Human)
Description:EBI_217
Residue:467
Sequence:
MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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Component 2
Name:Gamma-aminobutyric acid receptor subunit beta-3
Synonyms:GABA A receptor alpha-4/beta-3/gamma-2 | GABA receptor beta-3 subunit | GABA-A receptor | GABRB3 | GBRB3_HUMAN | agonist GABA site
Type:PROTEIN
Mol. Mass.:54130.51
Organism:Homo sapiens (Human)
Description:ChEMBL_448071
Residue:473
Sequence:
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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Component 3
Name:Gamma-aminobutyric acid receptor subunit alpha-5
Synonyms:GABA receptor alpha-5 subunit | GABA(A) receptor subunit alpha-5 (GABAAa5) | GABRA5 | GBRA5_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-5 (GABA(A)) | Gamma-aminobutyric acid receptor subunit alpha-5 (GABAA)
Type:Enzyme
Mol. Mass.:52160.59
Organism:Homo sapiens (Human)
Description:P31644
Residue:462
Sequence:
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN
SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
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BDBM50143088
n/a
NameBDBM50143088
Synonyms:3-Phenyl-6-(pyrimidin-4-ylmethoxy)-[1,2,4]triazolo[3,4-a]phthalazine | CHEMBL292380
TypeSmall organic molecule
Emp. Form.C20H14N6O
Mol. Mass.354.3648
SMILESC(Oc1nn2c(nnc2c2ccccc12)-c1ccccc1)c1ccncn1
Structure
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