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Target
Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2
Ligand
BDBM50122841
Substrate
n/a
Meas. Tech.
ChEMBL_70706 (CHEMBL685342)
Ki
223±n/a nM
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 Chem 46:310-3 (2003) [PubMed]  Article 
Target
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:
MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
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:
MDNGMLSRFIMTKTLLVFCISMTLSSHFGFSQMPTSSVQDETNDNITIFTRILDGLLDGYDNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPLNNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDFPMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTSTGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAAKIKKKERELILNKSTNAFTTGKLTHPPNIPKEQLPGGTGNAVGTASIRASEEKTSESKKTYNSISKIDKMSRIVFPILFGTFNLVYWATYLNREPVIKGATSPK
  
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:
MWGFAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPPVCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSEINRVDAHGNILLAPMDVHNEMNEVAGSVGDTRNSAISFDNSGIQYRKQSMPKEGHGRYMGDRSIPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
  
Inhibitor
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:
Search PDB for entries with ligand similarity: