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TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
LigandBDBM50207314
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1630656 (CHEMBL3873362)
EC50 238±n/a nM
Citation Marcinkowska, MKolaczkowski, MKaminski, KBucki, APawlowski, MSiwek, AKarcz, TMordyl, BStarowicz, GKubowicz, PPekala, EWesolowska, ASamochowiec, JMierzejewski, PBienkowski, P Design, synthesis, and biological evaluation of fluorinated imidazo[1,2-a]pyridine derivatives with potential antipsychotic activity. Eur J Med Chem124:456-467 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
Name:Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2
Synonyms:GABA receptor alpha-1/beta-2/gamma-2 subunit | GABA-A receptor; alpha-1/beta-2/gamma-2
Type:Protein
Mol. Mass.:n/a
Description:n/a
Components:This complex has 3 components.
Component 1
Name:Gamma-aminobutyric acid receptor subunit alpha-1
Synonyms:Benzodiazepine central | GABA A Benzodiazepine brain | GABA A Benzodiazepine liver | GABA receptor alpha-1 subunit | GABA(A) receptor subunit alpha-1 | GABA-A | GABA-A receptor | GABRA1 | GBRA1_HUMAN | Gamma-aminobutyric acid receptor subunit alpha (GABAA) | TBPS | agonist GABA site
Type:Protein
Mol. Mass.:51817.35
Organism:Homo sapiens (Human)
Description:P14867
Residue:456
Sequence:
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
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Component 2
Name:Gamma-aminobutyric acid receptor subunit beta-2
Synonyms:GABA(A) receptor subunit beta-2 | GABRB2 | GBRB2_HUMAN
Type:PROTEIN
Mol. Mass.:59167.91
Organism:Homo sapiens (Human)
Description:EBI_221
Residue:512
Sequence:
MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKI
FYKDIKQNGTQYRSLWDPTGNLSPTRRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEA
VMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPD
LTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
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Component 3
Name:Gamma-aminobutyric acid receptor subunit gamma-2
Synonyms:GABA(A) receptor subunit gamma-2 | GABRG2 | GBRG2_HUMAN
Type:PROTEIN
Mol. Mass.:54172.74
Organism:Homo sapiens (Human)
Description:EBI_217
Residue:467
Sequence:
MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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BDBM50207314
n/a
NameBDBM50207314
Synonyms:CHEMBL3971200
TypeSmall organic molecule
Emp. Form.C18H18FN3O
Mol. Mass.311.3534
SMILESCN(C)C(=O)Cc1c(nc2ccc(C)cn12)-c1ccc(F)cc1
Structure
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