Reaction Details |
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Target | GABA-A receptor; alpha-2/beta-3/gamma-2 |
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Ligand | BDBM50143088 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_69648 (CHEMBL681841) |
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Ki | 2.9±n/a nM |
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Citation | Carling, RW; Moore, KW; Street, LJ; Wild, D; Isted, C; Leeson, PD; Thomas, S; O'Connor, D; McKernan, RM; Quirk, K; Cook, SM; Atack, JR; Wafford, KA; Thompson, SA; Dawson, GR; Ferris, P; Castro, JL 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. J Med Chem47:1807-22 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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GABA-A receptor; alpha-2/beta-3/gamma-2 |
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Name: | GABA-A receptor; alpha-2/beta-3/gamma-2 |
Synonyms: | GABA receptor alpha-2/beta-3/gamma-2 subunit | Gamma-aminobutyric acid receptor subunit alpha-2/beta-3/gamma-2 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 2148174 |
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-2 |
Synonyms: | GABA receptor alpha-2 subunit | GABRA2 | GBRA2_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2) |
Type: | Protein |
Mol. Mass.: | 51338.78 |
Organism: | Homo sapiens (Human) |
Description: | P47869 |
Residue: | 451 |
Sequence: | MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC
PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM
TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASV
MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM
SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
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BDBM50143088 |
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n/a |
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Name | BDBM50143088 |
Synonyms: | 3-Phenyl-6-(pyrimidin-4-ylmethoxy)-[1,2,4]triazolo[3,4-a]phthalazine | CHEMBL292380 |
Type | Small organic molecule |
Emp. Form. | C20H14N6O |
Mol. Mass. | 354.3648 |
SMILES | C(Oc1nn2c(nnc2c2ccccc12)-c1ccccc1)c1ccncn1 |
Structure |
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