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Target
Gamma-aminobutyric acid receptor subunit alpha-4
Ligand
BDBM235901
Substrate
n/a
Meas. Tech.
[35S]-TBPS Displacement Assay
IC50
43±3 nM
Citation
 Covey, D Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptors US Patent  US9365502 Publication Date 6/14/2016 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-4
Synonyms:
GBRA4_RAT | Gabra4 | Gamma-aminobutyric acid receptor (GABA(A)) subunit alpha-4
Type:
Enzyme
Mol. Mass.:
60972.37
Organism:
Rattus norvegicus (Rat)
Description:
P28471
Residue:
552
Sequence:
MVSVQKVPAIVLCSGVSLALLHVLCLATCLNESPGQNSKDEKLCPENFTRILDSLLDGYDNRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLNNMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFPMDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSITGEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMQKAKKKISKPPPEVPAAPVLKEKHTETSLQNTHANLNMRKRTNALVHSESDVNSRTEVGNHSSKTTAAQESSETTPKAHLASSPNPFSRANAAETISAAARGLSSAASPSPHGTLQPAPLRSASARPAFGARLGRIKTTVNTTGVPGNVSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVVYLSKDTMEKSESLM
  
Inhibitor
Name:
BDBM235901
Synonyms:
US9365502, MQ-86
Type:
Small organic molecule
Emp. Form.:
C20H29NO
Mol. Mass.:
299.4504
SMILES:
C[C@]12C[C@H]3CC[C@@H]4C[C@@H](O)CC[C@@]4(C)C3CC1CC=C2C#N |r,c:21|
Structure:
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