Target
Gamma-aminobutyric acid receptor subunit alpha-4
Ligand
BDBM50244261
Substrate
n/a
Meas. Tech.
ChEMBL_491124 (CHEMBL991892)
Ki
2.61±n/a nM
Citation
 Harris, DClayton, TCook, JSahbaie, PHalliwell, RFFurtmüller, RHuck, SSieghart, WDeLorey, TM Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit. J Med Chem 51:3788-803 (2008) [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:
BDBM50244261
Synonyms:
5-Methyl-6-oxo-8-trimethylsilanylethynyl-3a,4,5,6-tetrahydro-1H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid tert-butyl ester | CHEMBL471977
Type:
Small organic molecule
Emp. Form.:
C22H29N3O3Si
Mol. Mass.:
411.5695
SMILES:
CN1CC2N(CN=C2C(=O)OC(C)(C)C)c2ccc(cc2C1=O)C#C[Si](C)(C)C |c:6|
Structure:
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