Reaction Details |
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Target | Glutamate receptor ionotropic, kainate 1 |
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Ligand | BDBM50200526 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1652084 (CHEMBL4001339) |
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Ki | 50±n/a nM |
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Citation | Krogsgaard-Larsen, N; Delgar, CG; Koch, K; Brown, PM; Møller, C; Han, L; Huynh, TH; Hansen, SW; Nielsen, B; Bowie, D; Pickering, DS; Kastrup, JS; Frydenvang, K; Bunch, L Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidin J Med Chem60:441-457 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glutamate receptor ionotropic, kainate 1 |
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Name: | Glutamate receptor ionotropic, kainate 1 |
Synonyms: | GLUR5 | GRIK1 | GRIK1_HUMAN | Glutamate Receptor | Glutamate kainate | Glutamate receptor ionotropic kainate | Glutamate receptor ionotropic kainate 1 | Glutamate receptor, ionotropic kainate 1 | Glutamate-Kainate | Glutamate-Kainate, GluR5 | Grik1 protein | hmglur5 flipr |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 103984.96 |
Organism: | Homo sapiens (Human) |
Description: | P39086 |
Residue: | 918 |
Sequence: | MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKF
AVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQ
SICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDS
TGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEIL
KQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSME
RLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRF
MNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGI
WNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCL
DLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREK
VIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFT
PYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTL
IIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKM
WAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYG
VGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFI
VLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECG
KLIREERGIRKQSSVHTV
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BDBM50200526 |
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n/a |
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Name | BDBM50200526 |
Synonyms: | CHEMBL1234118 |
Type | Small organic molecule |
Emp. Form. | C16H24F2N2O4 |
Mol. Mass. | 346.3696 |
SMILES | OC(=O)[C@@H]1CC(F)(F)CN1C[C@H]1CC[C@H]2CN[C@@H](C[C@H]2C1)C(O)=O |r| |
Structure |
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