Reaction Details |
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Target | GABA-A receptor; alpha-5/beta-3/gamma-2 |
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Ligand | BDBM50179927 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_340231 (CHEMBL862572) |
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Ki | 0.5±n/a nM |
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Citation | Jennings, AS; Lewis, RT; Russell, MG; Hallett, DJ; Street, LJ; Castro, JL; Atack, JR; Cook, SM; Lincoln, R; Stanley, J; Smith, AJ; Reynolds, DS; Sohal, B; Pike, A; Marshall, GR; Wafford, KA; Sheppard, WF; Tye, SJ Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety. Bioorg Med Chem Lett16:1477-80 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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GABA-A receptor; alpha-5/beta-3/gamma-2 |
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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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BDBM50179927 |
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n/a |
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Name | BDBM50179927 |
Synonyms: | 2-(7-(4-fluoro-3-(pyridin-4-yl)phenyl)imidazo[1,2-b][1,2,4]triazin-3-yl)propan-2-ol | CHEMBL204156 |
Type | Small organic molecule |
Emp. Form. | C19H16FN5O |
Mol. Mass. | 349.3616 |
SMILES | CC(C)(O)c1cnn2c(cnc2n1)-c1ccc(F)c(c1)-c1ccncc1 |
Structure |
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