| Reaction Details |
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 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2 |
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| Ligand | BDBM50122843 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_70706 (CHEMBL685342) |
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| Ki | 207±n/a nM |
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| Citation |  Selleri, S; Bruni, F; Costagli, C; Costanzo, A; Guerrini, G; Ciciani, G; Gratteri, P; Bonaccini, C; Malmberg Aiello, P; Besnard, F; Renard, S; Costa, B; Martini, C Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. J Med Chem46:310-3 (2003) [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-5/beta-3/gamma-2 |
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| Name: | Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2 |
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| Synonyms: | GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5/beta-3/gamma-2 subunit |
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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 70706 |
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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: | GBRG2_RAT | Gabrg2 | Gamma-aminobutyric acid receptor subunit gamma-2 (GABA(A) gamma-2) |
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| Type: | Enzyme |
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| Mol. Mass.: | 54087.63 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P18508 |
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| Residue: | 466 |
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| Sequence: | MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKV
PEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTW
YDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYT
LRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFS
FVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAV
PARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVS
NRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCF
EDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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| Component 2 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-5 |
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| Synonyms: | GABA A Alpha5Beta2Gamma2 | GABA A Alpha5Beta3Gamma2 | GABA A Alpha5m10Beta2Gamma2 | GABA A Alpha5m8Beta2Gamma2 | GABA A Alpha5m9Beta2Gamma2 | GABA A alpha5 | GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5 subunit | GBRA5_RAT | Gabra-5 | Gabra5 | Gamma-aminobutyric acid receptor subunit alpha-5 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 52350.79 |
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| Organism: | RAT |
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| Description: | GABA A alpha5 0 RAT::P19969 |
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| Residue: | 464 |
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| Sequence: | MDNGMLSRFIMTKTLLVFCISMTLSSHFGFSQMPTSSVQDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKERELILNKSTNAFTTGKLTHPPNIPKEQLPGGTGNAVGTASIRASEEKTSESKKT
YNSISKIDKMSRIVFPILFGTFNLVYWATYLNREPVIKGATSPK
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| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-3 |
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| Synonyms: | GABA receptor beta-3 subunit | GBRB3_RAT | Gabrb-3 | Gabrb3 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 54180.66 |
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| Organism: | Rattus norvegicus |
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| Description: | EBI_12481 |
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| Residue: | 473 |
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| Sequence: | MWGFAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSEINR
VDAHGNILLAPMDVHNEMNEVAGSVGDTRNSAISFDNSGIQYRKQSMPKEGHGRYMGDRS
IPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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| BDBM50122843 |
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| n/a |
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| Name | BDBM50122843 |
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| Synonyms: | 6-Thiophen-3-yl-3-(3-trifluoromethyl-phenyl)-4H-pyrazolo[1,5-a]pyrimidin-7-one | CHEMBL322313 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H10F3N3OS |
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| Mol. Mass. | 361.341 |
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| SMILES | FC(F)(F)c1cccc(c1)-c1c[nH]n2c1ncc(-c1ccsc1)c2=O |
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| Structure | 
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