| 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 | BDBM50185487 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_373310 (CHEMBL853517) |
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| Ki | 8.7±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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| BDBM50185487 |
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| n/a |
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| Name | BDBM50185487 |
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| Synonyms: | 3-(2-chlorophenyl)-7-(2-fluorophenyl)-2-((2-methyl-2H-1,2,4-triazol-3-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazine | CHEMBL212052 |
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| Type | Small organic molecule |
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| Emp. Form. | C21H15ClFN7O |
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| Mol. Mass. | 435.842 |
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| SMILES | Cn1ncnc1COc1nn2c(nncc2c1-c1ccccc1Cl)-c1ccccc1F |(24.31,-2.56,;22.84,-2.09,;21.6,-3,;20.35,-2.1,;20.82,-.63,;22.37,-.62,;23.14,.71,;24.68,.7,;25.46,2.04,;26.99,2.19,;27.32,3.7,;28.66,4.47,;28.66,6.02,;27.31,6.79,;25.99,6.01,;25.98,4.48,;24.83,3.45,;23.5,4.21,;23.5,5.75,;22.17,6.51,;20.83,5.74,;20.84,4.19,;22.18,3.43,;22.19,1.89,;30,3.7,;29.99,2.16,;31.33,1.39,;32.66,2.17,;32.65,3.71,;31.32,4.47,;31.31,6.01,)| |
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| Structure | 
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