| Reaction Details |
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 | Report a problem with these data |
| Target | Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit |
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| Ligand | BDBM50509858 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1839472 (CHEMBL4339687) |
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| IC50 | 1259±n/a nM |
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| Citation |  Savall, BM; Wu, D; Swanson, DM; Seierstad, M; Wu, N; Vives Martinez, J; García Olmos, B; Lord, B; Coe, K; Koudriakova, T; Lovenberg, TW; Carruthers, NI; Maher, MP; Ameriks, MK Discovery of Imidazo[1,2- ACS Med Chem Lett10:267-272 (2019) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit |
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| Name: | Glutamate receptor 1/Voltage-dependent calcium channel gamma-2 subunit |
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| Synonyms: | GRIA1/CACNG2 |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 1839473 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Glutamate receptor 1 |
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| Synonyms: | AMPA-selective glutamate receptor 1 | GLUH1 | GLUR1 | GRIA1 | GRIA1_HUMAN | GluR-1 | GluR-A | GluR-K1 | Glutamate AMPA 1 | Glutamate receptor 1 | Glutamate receptor AMPA 1/2 | Glutamate receptor ionotropic AMPA | Glutamate receptor ionotropic, AMPA 1 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 101512.92 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Glutamate AMPA 1 GRIA1 HUMAN::P42261 |
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| Residue: | 906 |
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| Sequence: | MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQID
IVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQ
FVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTT
TEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDL
NKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVM
AEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGR
RTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYV
MLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGE
LVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIW
MCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQ
QGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIA
YGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLES
TMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKW
WYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMK
GFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMP
LGATGL
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| Component 2 |
| Name: | Voltage-dependent calcium channel gamma-2 subunit |
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| Synonyms: | CACNG2 | CCG2_HUMAN | Neuronal voltage-gated calcium channel gamma-2 subunit | TARP gamma-2 | Transmembrane AMPAR regulatory protein gamma-2 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 35977.54 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 323 |
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| Sequence: | MGLFDRGVQMLLTTVGAFAAFSLMTIAVGTDYWLYSRGVCKTKSVSENETSKKNEEVMTH
SGLWRTCCLEGNFKGLCKQIDHFPEDADYEADTAEYFLRAVRASSIFPILSVILLFMGGL
CIAASEFYKTRHNIILSAGIFFVSAGLSNIIGIIVYISANAGDPSKSDSKKNSYSYGWSF
YFGALSFIIAEMVGVLAVHMFIDRHKQLRATARATDYLQASAITRIPSYRYRYQRRSRSS
SRSTEPSHSRDASPVGIKGFNTLPSTEISMYTLSRDPLKAATTPTATYNSDRDNSFLQVH
NCIQKENKDSLHSNTANRRTTPV
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| BDBM50509858 |
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| n/a |
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| Name | BDBM50509858 |
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| Synonyms: | CHEMBL4526929 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H13FN2O |
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| Mol. Mass. | 304.3177 |
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| SMILES | Oc1ccc(cc1)-n1c(nc2ccccc12)-c1ccc(F)cc1 |
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| Structure | 
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