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Target
Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/delta
Ligand
BDBM50457439
Substrate
n/a
Meas. Tech.
ChEMBL_1759688 (CHEMBL4194696)
EC50
130±n/a nM
Citation
 Yakoub, K; Jung, S; Sattler, C; Damerow, H; Weber, J; Kretzschmann, A; Cankaya, AS; Piel, M; Rösch, F; Haugaard, AS; Frølund, B; Schirmeister, T; Lüddens, H Structure-Function Evaluation of Imidazopyridine Derivatives Selective for ?-Subunit-Containing ?-Aminobutyric Acid Type A (GABA J Med Chem 61:1951-1968 (2018) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-6/beta-2/delta
Synonyms:
n/a
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1759656
Components:
This complex has 3 components.
Component 1
Name:
Gamma-aminobutyric acid receptor subunit delta
Synonyms:
GABA(A) receptor subunit delta | GBRD_RAT | Gabrd
Type:
Enzyme
Mol. Mass.:
50571.23
Organism:
Rattus norvegicus (Rat)
Description:
P18506
Residue:
449
Sequence:
MDVLGWLLLPLLLLCTQPHHGARAMNDIGDYVGSNLEISWLPNLDGLMEGYARNFRPGIGGPPVNVALALEVASIDHISEANMEYTMTVFLHQSWRDSRLSYNHTNETLGLDSRFVDKLWLPDTFIVNAKSAWFHDVTVENKLIRLQPDGVILYSIRITSTVACDMDLAKYPMDEQECMLDLESYGYSSEDIVYYWSENQEQIHGLDRLQLAQFTITSYRFTTELMNFKSAGQFPRLSLHFQLRRNRGVYIIQSYMPSVLLVAMSWVSFWISQAAVPARVSLGITTVLTMTTLMVSARSSLPRASAIKALDVYFWICYVFVFAALVEYAFAHFNADYRKKRKAKVKVTKPRAEMDVRNAIVLFSLSAAGVSQELAISRRQGRVPGNLMGSYRSVEVEAKKEGGSRPGGPGGIRSRLKPIDADTIDIYARAVFPAAFAAVNIIYWAAYTM
  
Component 2
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 3
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
  
Inhibitor
Name:
BDBM50457439
Synonyms:
CHEMBL4213357
Type:
Small organic molecule
Emp. Form.:
C18H10Br2ClN3OS
Mol. Mass.:
511.618
SMILES:
Clc1ccc(cc1)C(=O)Nc1c(nc2c(Br)cc(Br)cn12)-c1cccs1
Structure:
Search PDB for entries with ligand similarity: