Reaction Details |
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Target | Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2 |
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Ligand | BDBM50122841 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70706 (CHEMBL685342) |
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Ki | 223±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 |
Synonyms: | GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5/beta-3/gamma-2 subunit |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 70706 |
Components: | This complex has 3 components. |
Component 1 |
Name: | Gamma-aminobutyric acid receptor subunit gamma-2 |
Synonyms: | GBRG2_RAT | Gabrg2 | Gamma-aminobutyric acid receptor subunit gamma-2 (GABA(A) gamma-2) |
Type: | Enzyme |
Mol. Mass.: | 54087.63 |
Organism: | Rattus norvegicus (Rat) |
Description: | P18508 |
Residue: | 466 |
Sequence: | MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKV
PEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTW
YDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYT
LRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFS
FVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAV
PARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVS
NRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCF
EDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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Component 2 |
Name: | Gamma-aminobutyric acid receptor subunit alpha-5 |
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 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 52350.79 |
Organism: | RAT |
Description: | GABA A alpha5 0 RAT::P19969 |
Residue: | 464 |
Sequence: | MDNGMLSRFIMTKTLLVFCISMTLSSHFGFSQMPTSSVQDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKERELILNKSTNAFTTGKLTHPPNIPKEQLPGGTGNAVGTASIRASEEKTSESKKT
YNSISKIDKMSRIVFPILFGTFNLVYWATYLNREPVIKGATSPK
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Component 3 |
Name: | Gamma-aminobutyric acid receptor subunit beta-3 |
Synonyms: | GABA receptor beta-3 subunit | GBRB3_RAT | Gabrb-3 | Gabrb3 |
Type: | PROTEIN |
Mol. Mass.: | 54180.66 |
Organism: | Rattus norvegicus |
Description: | EBI_12481 |
Residue: | 473 |
Sequence: | MWGFAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSEINR
VDAHGNILLAPMDVHNEMNEVAGSVGDTRNSAISFDNSGIQYRKQSMPKEGHGRYMGDRS
IPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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BDBM50122841 |
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n/a |
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Name | BDBM50122841 |
Synonyms: | 3-(3H-1lambda*4*-Thiophen-3-yl)-6-thiophen-3-yl-4H-pyrazolo[1,5-a]pyrimidin-7-one | CHEMBL322697 |
Type | Small organic molecule |
Emp. Form. | C14H9N3OS2 |
Mol. Mass. | 299.371 |
SMILES | O=c1c(cnc2c(c[nH]n12)-c1ccsc1)-c1ccsc1 |
Structure |
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