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Target
Gamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2
Ligand
BDBM50122841
Substrate
n/a
Meas. Tech.
ChEMBL_70392 (CHEMBL683018)
Ki
196±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-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:
MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAANANNEKMRLDVNKMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
  
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:
MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
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:
MITTQMWHFYVTRVGLLLLISILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDSTDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQTWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLLYTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTKAEVIYSWTLGKNKSVEVAQDGSRLNQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFMAVCYAFVFSALIEFATVNYFTKRSWAWEGKKVPEALEMKKKTPAAPTKKTSTTFNIVGTTYPINLALDTEFSTISKAAAAPSASSTPTVIASPKTTYVQDSPAETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVNRESAIKGMIRKQ
  
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: