Target
Gamma-aminobutyric acid receptor subunit alpha-4
Ligand
BDBM50049736
Substrate
n/a
Meas. Tech.
ChEMBL_491428 (CHEMBL948523)
EC50
324400±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:
BDBM50049736
Synonyms:
8-Ethynyl-5-methyl-6-oxo-5,6-dihydro-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid tert-butyl ester | 8-Ethynyl-5-methyl-6-oxo-5,6-dihydro-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid tert-butyl ester(RY 24) | CHEMBL58757
Type:
Small organic molecule
Emp. Form.:
C19H19N3O3
Mol. Mass.:
337.3725
SMILES:
CN1Cc2c(ncn2-c2ccc(cc2C1=O)C#C)C(=O)OC(C)(C)C
Structure:
Search PDB for entries with ligand similarity: