| 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 | BDBM50185504 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_373310 (CHEMBL853517) |
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| Ki | 21±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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| BDBM50185504 |
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| n/a |
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| Name | BDBM50185504 |
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| Synonyms: | 7-(2-chlorophenyl)-3-(2-fluorophenyl)-2-((2-methyl-2H-1,2,4-triazol-3-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazine | CHEMBL377533 |
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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-c1ccccc1F)-c1ccccc1Cl |(-6.02,-19.33,;-7.55,-19.11,;-8.62,-20.21,;-10,-19.53,;-9.79,-18.01,;-8.26,-17.74,;-7.49,-16.41,;-8.25,-15.07,;-7.48,-13.74,;-5.94,-13.59,;-5.61,-12.08,;-4.27,-11.31,;-4.28,-9.76,;-5.62,-8.99,;-6.94,-9.76,;-6.95,-11.3,;-8.1,-12.33,;-9.43,-11.57,;-9.43,-10.03,;-10.76,-9.26,;-12.1,-10.04,;-12.09,-11.59,;-10.75,-12.35,;-10.74,-13.89,;-2.94,-12.08,;-2.94,-13.62,;-1.61,-14.38,;-.27,-13.61,;-.28,-12.06,;-1.61,-11.3,;-1.62,-9.76,)| |
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| Structure | 
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