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Target
Gamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2
Ligand
BDBM50122845
Substrate
n/a
Meas. Tech.
ChEMBL_37810 (CHEMBL651185)
Ki
827.0±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-2/beta-2/gamma-2
Synonyms:
GABA receptor alpha-2/beta-2/gamma-2 subunit
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 37810
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-2
Synonyms:
GABA A Alpha2Beta2Gamma2 | GABA A alpha2 | GABA A receptor alpha-2/beta-2/gamma-2 | GABA receptor alpha-2 subunit | GABA(A) receptor subunit alpha-2 | GBRA2_RAT | Gabra-2 | Gabra2 | Gamma-aminobutyric acid receptor subunit alpha-2
Type:
Enzyme
Mol. Mass.:
51195.57
Organism:
Rattus norvegicus (Rat)
Description:
P23576
Residue:
451
Sequence:
MRTKLSTCNVWFPLLVLLVWNPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPGLGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNSMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSCPLKFGSYAYTTSEVTYIWTYNPSDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKGSVMIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRMSRIVFPVLFGTFNLVYWATYLNREPVLGVSP
  
Inhibitor
Name:
BDBM50122845
Synonyms:
3-(3-Methoxy-phenyl)-6-thiophen-3-yl-4H-pyrazolo[1,5-a]pyrimidin-7-one | CHEMBL107447
Type:
Small organic molecule
Emp. Form.:
C17H13N3O2S
Mol. Mass.:
323.369
SMILES:
COc1cccc(c1)-c1c[nH]n2c1ncc(-c1ccsc1)c2=O
Structure:
Search PDB for entries with ligand similarity: