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Target
Gamma-aminobutyric acid receptor subunit alpha-4
Ligand
BDBM50142570
Substrate
n/a
Meas. Tech.
ChEBML_32535
Ki
28±n/a nM
Citation
 Crawforth, J; Atack, JR; Cook, SM; Gibson, KR; Nadin, A; Owens, AP; Pike, A; Rowley, M; Smith, AJ; Sohal, B; Sternfeld, F; Wafford, K; Street, LJ Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands. Bioorg Med Chem Lett 14:1679-82 (2004) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-4
Synonyms:
GABA A Alpha4Beta2Gamma2 | GABA A Alpha4Beta3Gamma2 | GABA A Alpha4Gamma2 | GABA A receptor alpha-4/beta-3/gamma-2 | GABA receptor alpha-4 subunit | GABA(A) receptor subunit alpha-4 | GABRA4 | GBRA4_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-4
Type:
Enzyme Catalytic Domain
Mol. Mass.:
61648.70
Organism:
Homo sapiens (Human)
Description:
GABA A Alpha4Beta2Gamma2 0 HUMAN::P48169
Residue:
554
Sequence:
MVSAKKVPAIALSAGVSFALLRFLCLAVCLNESPGQNQKEEKLCTENFTRILDSLLDGYDNRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLNNMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFPMDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSITGEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMEKAKRKTSKPPQEVPAAPVQREKHPEAPLQNTNANLNMRKRTNALVHSESDVGNRTEVGNHSSKSSTVVQESSKGTPRSYLASSPNPFSRANAAETISAARALPSASPTSIRTGYMPRKASVGSASTRHVFGSRLQRIKTTVNTIGATGKLSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVVYLSKDTMEKSESLM
  
Inhibitor
Name:
BDBM50142570
Synonyms:
9-(4-Methyl-thiazol-2-yl)-11-pyridin-4-yl-6,7-dihydro-5H-2,7a-diaza-dibenzo[a,c]cyclohepten-8-one | CHEMBL45198
Type:
Small organic molecule
Emp. Form.:
C22H18N4OS
Mol. Mass.:
386.47
SMILES:
Cc1csc(n1)-c1cc(-c2ccncc2)c2-c3cnccc3CCCn2c1=O
Structure:
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