Reaction Details |
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Target | Gamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2 |
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Ligand | BDBM50122840 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70392 (CHEMBL683018) |
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Ki | 111±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-3/beta-2/gamma-2 |
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Name: | Gamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2 |
Synonyms: | GABA A receptor alpha-3/beta-2/gamma-2 | GABA receptor alpha-3/beta-2/gamma-2 subunit |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 68412 |
Components: | This complex has 3 components. |
Component 1 |
Name: | Gamma-aminobutyric acid receptor subunit beta-2 |
Synonyms: | GBRB2_RAT | Gabrb-2 | Gabrb2 | Gamma-aminobutyric acid receptor subunit beta-2 (GABA(A) beta-2) |
Type: | Enzyme |
Mol. Mass.: | 54648.97 |
Organism: | Rattus norvegicus (Rat) |
Description: | P63138 |
Residue: | 474 |
Sequence: | MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAANANNEKMRLDVNKM
DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER
HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
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Component 2 |
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 3 |
Name: | Gamma-aminobutyric acid receptor subunit alpha-3 |
Synonyms: | GABA A anti-Alpha3 | GABA A receptor alpha-3/beta-2/gamma-2 | GABA receptor alpha-3 subunit | GBRA3_RAT | Gabra-3 | Gabra3 | Gamma-aminobutyric acid receptor subunit alpha-3 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 55444.88 |
Organism: | RAT |
Description: | GABA A Alpha3Beta2Gamma2 0 RAT::P20236 |
Residue: | 493 |
Sequence: | MITTQMWHFYVTRVGLLLLISILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTKAEVIYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFMAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPTKKTSTTFNIVGTTYPINLALDTEFSTISKAA
AAPSASSTPTVIASPKTTYVQDSPAETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYV
NRESAIKGMIRKQ
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BDBM50122840 |
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n/a |
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Name | BDBM50122840 |
Synonyms: | 3-(3-Bromo-phenyl)-6-thiophen-3-yl-4H-pyrazolo[1,5-a]pyrimidin-7-one | CHEMBL440150 |
Type | Small organic molecule |
Emp. Form. | C16H10BrN3OS |
Mol. Mass. | 372.239 |
SMILES | Brc1cccc(c1)-c1c[nH]n2c1ncc(-c1ccsc1)c2=O |
Structure |
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