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Target
Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/gamma-2
Ligand
BDBM50026756
Substrate
n/a
Meas. Tech.
ChEMBL_217781 (CHEMBL824042)
Ki
>10000±n/a nM
Citation
 Wieland, HA; Lüddens, H Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem 37:4576-80 (1995) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/gamma-2
Synonyms:
GABA A receptor alpha-6/beta-2/gamma-2 | GABA receptor alpha-6/beta-2/gamma-2 subunit
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 70244
Components:
This complex has 3 components.
Component 1
Name:
Gamma-aminobutyric acid receptor subunit alpha-6
Synonyms:
GABA A Alpha6Beta3Gamma2 | GABA A receptor alpha-6/beta-2/gamma-2 | GABA receptor alpha-6 subunit | GBRA6_RAT | Gabra-6 | Gabra6 | Gamma-aminobutyric acid receptor subunit alpha-6
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51188.24
Organism:
RAT
Description:
GABA A Alpha6Beta2Gamma2 0 RAT::P30191
Residue:
453
Sequence:
MLLLLPWLFSLLWIENAQAQLEDEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFKGPAEILSLNNLMVSKIWTPDTFFRNGKKSIAHNMTTPNKLFRLMHNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYPKSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKMGYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNLQSQKAERQAQTAAKPPVAKSKTTESLEAEIVVHSDSKYHLKKRISSLTLPIVPSSEASKVLSRTPILPSTPVTPPLLLPAIGGTSKIDQYSRILFPVAFAGFNLVYWIVYLSKDTMEVSSTVE
  
Component 2
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 3
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
  
Inhibitor
Name:
BDBM50026756
Synonyms:
3-Methyl-6-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[4,3-b]pyridazine | CHEMBL13662 | CI-218872 | CL 218872 | CL218,872 | v3-Methyl-6-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[4,3-b]pyridazine
Type:
Small organic molecule
Emp. Form.:
C13H9F3N4
Mol. Mass.:
278.2326
SMILES:
Cc1nnc2ccc(nn12)-c1cccc(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: