Reaction Details |
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Target | GABA A receptor alpha-4/beta-3/gamma-2 |
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Ligand | BDBM24183 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_70537 (CHEMBL681094) |
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EC50 | 50000±n/a nM |
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Citation | Ebert, B; Mortensen, M; Thompson, SA; Kehler, J; Wafford, KA; Krogsgaard-Larsen, P Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors. Bioorg Med Chem Lett11:1573-7 (2001) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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GABA A receptor alpha-4/beta-3/gamma-2 |
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Name: | GABA A receptor alpha-4/beta-3/gamma-2 |
Synonyms: | GABA receptor alpha-4/beta-3/gamma-2 subunit | Gamma-aminobutyric acid receptor subunit alpha-4/beta-3/gamma-2 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 2148176 |
Components: | This complex has 3 components. |
Component 1 |
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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Component 2 |
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: | Homo sapiens (Human) |
Description: | ChEMBL_448071 |
Residue: | 473 |
Sequence: | MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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Component 3 |
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: | MVSAKKVPAIALSAGVSFALLRFLCLAVCLNESPGQNQKEEKLCTENFTRILDSLLDGYD
NRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLN
NMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFP
MDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSIT
GEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMT
TLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMEKAKRKTSKPPQ
EVPAAPVQREKHPEAPLQNTNANLNMRKRTNALVHSESDVGNRTEVGNHSSKSSTVVQES
SKGTPRSYLASSPNPFSRANAAETISAARALPSASPTSIRTGYMPRKASVGSASTRHVFG
SRLQRIKTTVNTIGATGKLSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVV
YLSKDTMEKSESLM
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BDBM24183 |
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n/a |
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Name | BDBM24183 |
Synonyms: | 4-amino-n-[2,3-3H]butyric acid | 4-aminobutanoic acid | Aminalon | CHEMBL96 | GABA | Gamma-Aminobutyric acid | [3H]GABA | cid_119 |
Type | Radiolabeled ligand |
Emp. Form. | C4H9NO2 |
Mol. Mass. | 103.1198 |
SMILES | NCCCC(O)=O |
Structure |
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