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Target
Gamma-aminobutyric acid receptor subunit alpha-4/beta-3/delta
Ligand
BDBM50258249
Substrate
n/a
Meas. Tech.
ChEMBL_1690286 (CHEMBL4040856)
EC50
2012±n/a nM
Citation
Martinez Botella, G; Salituro, FG; Harrison, BL; Beresis, RT; Bai, Z; Blanco, MJ; Belfort, GM; Dai, J; Loya, CM; Ackley, MA; Althaus, AL; Grossman, SJ; Hoffmann, E; Doherty, JJ; Robichaud, AJ Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid) J Med Chem 60:7810-7819 (2017) [PubMed] Article
More Info.:
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-4/beta-3/delta
Synonyms:
Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1690286
Components:
This complex has 3 components.
Component 1
Name:
Gamma-aminobutyric acid receptor subunit beta-3
Synonyms:
GABA A receptor alpha-4/beta-3/gamma-2 | GABA receptor beta-3 subunit | GABA-A receptor | GABRB3 | GBRB3_HUMAN | agonist GABA site
Type:
PROTEIN
Mol. Mass.:
54130.51
Organism:
Human
Description:
ChEMBL_448071
Residue:
473
Sequence:
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPPVCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNRVDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRSLPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
Component 2
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:
Human
Description:
GABA A Alpha4Beta2Gamma2 0 HUMAN::P48169
Residue:
554
Sequence:
MVSAKKVPAIALSAGVSFALLRFLCLAVCLNESPGQNQKEEKLCTENFTRILDSLLDGYDNRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLNNMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFPMDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSITGEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMEKAKRKTSKPPQEVPAAPVQREKHPEAPLQNTNANLNMRKRTNALVHSESDVGNRTEVGNHSSKSSTVVQESSKGTPRSYLASSPNPFSRANAAETISAARALPSASPTSIRTGYMPRKASVGSASTRHVFGSRLQRIKTTVNTIGATGKLSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVVYLSKDTMEKSESLM
Component 3
Name:
Gamma-aminobutyric acid receptor subunit delta
Synonyms:
GABA(A) receptor subunit delta | GABRD | GBRD_HUMAN | Gamma-aminobutyric acid receptor subunit delta
Type:
PROTEIN
Mol. Mass.:
50716.35
Organism:
Human
Description:
ChEMBL_109656
Residue:
452
Sequence:
MDAPARLLAPLLLLCAQQLRGTRAMNDIGDYVGSNLEISWLPNLDGLIAGYARNFRPGIGGPPVNVALALEVASIDHISEANMEYTMTVFLHQSWRDSRLSYNHTNETLGLDSRFVDKLWLPDTFIVNAKSAWFHDVTVENKLIRLQPDGVILYSIRITSTVACDMDLAKYPMDEQECMLDLESYGYSSEDIVYYWSESQEHIHGLDKLQLAQFTITSYRFTTELMNFKSAGQFPRLSLHFHLRRNRGVYIIQSYMPSVLLVAMSWVSFWISQAAVPARVSLGITTVLTMTTLMVSARSSLPRASAIKALDVYFWICYVFVFAALVEYAFAHFNADYRKKQKAKVKVSRPRAEMDVRNAIVLFSLSAAGVTQELAISRRQRRVPGNLMGSYRSVGVETGETKKEGAARSGGQGGIRARLRPIDADTIDIYARAVFPAAFAAVNVIYWAAYAM