| Reaction Details |
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 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2 |
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| Ligand | BDBM50185491 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_373310 (CHEMBL853517) |
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| Ki | 0.94±n/a nM |
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| Citation |  Carling, RW; Russell, MG; Moore, KW; Mitchinson, A; Guiblin, A; Smith, A; Wafford, KA; Marshall, G; Atack, JR; Street, LJ 2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists. Bioorg Med Chem Lett16:3550-4 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2 |
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| Name: | Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2 |
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| Synonyms: | GABA receptor alpha-3/beta-3/gamma-2 subunit | GABA-A receptor; alpha-3/beta-3/gamma-2 |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of EBI is 68410 |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Gamma-aminobutyric acid receptor subunit gamma-2 |
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| Synonyms: | GABA(A) receptor subunit gamma-2 | GABRG2 | GBRG2_HUMAN |
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| Type: | PROTEIN |
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| Mol. Mass.: | 54172.74 |
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| Organism: | Homo sapiens (Human) |
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| Description: | EBI_217 |
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| Residue: | 467 |
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| Sequence: | MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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| Component 2 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-3 |
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| Synonyms: | GABA A receptor alpha-4/beta-3/gamma-2 | GABA receptor beta-3 subunit | GABA-A receptor | GABRB3 | GBRB3_HUMAN | agonist GABA site |
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| Type: | PROTEIN |
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| Mol. Mass.: | 54130.51 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_448071 |
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| Residue: | 473 |
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| Sequence: | MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-3 |
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| Synonyms: | GABA A Alpha3Beta3Gamma2 | GABA A receptor alpha-3/beta-2/gamma-2 | GABA C | GABA receptor alpha-3 subunit | GABA-A receptor | GABRA3 | GBRA3_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-3 | agonist GABA site |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 55175.47 |
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| Organism: | Homo sapiens (Human) |
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| Description: | GABA A Alpha3Beta1Gamma2 0 HUMAN::P34903 |
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| Residue: | 492 |
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| Sequence: | MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
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| BDBM50185491 |
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| n/a |
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| Name | BDBM50185491 |
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| Synonyms: | 3-(2-fluorophenyl)-7-(4-fluorophenyl)-2-((2-methyl-2H-1,2,4-triazol-3-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazine | CHEMBL211293 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H15F2N7O |
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| Mol. Mass. | 419.3869 |
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| SMILES | Cn1ncnc1COc1nn2c(nncc2c1-c1ccccc1F)-c1ccc(F)cc1 |(9.57,-46.7,;8.04,-46.47,;6.97,-47.58,;5.59,-46.9,;5.8,-45.37,;7.33,-45.11,;8.1,-43.78,;7.34,-42.44,;8.11,-41.11,;9.65,-40.95,;9.98,-39.44,;11.32,-38.67,;11.31,-37.12,;9.97,-36.36,;8.65,-37.13,;8.64,-38.67,;7.49,-39.69,;6.16,-38.93,;6.16,-37.4,;4.83,-36.63,;3.49,-37.4,;3.5,-38.95,;4.84,-39.71,;4.85,-41.25,;12.65,-39.44,;12.65,-40.98,;13.98,-41.75,;15.32,-40.98,;16.65,-41.74,;15.31,-39.43,;13.98,-38.67,)| |
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| Structure | 
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