| Reaction Details |
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 | Report a problem with these data |
| Target | Glutamate receptor ionotropic, kainate 1 |
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| Ligand | BDBM50494060 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_990076 (CHEMBL2443753) |
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| Ki | 2300±n/a nM |
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| Citation |  Martinez-Perez, JA; Iyengar, S; Shannon, HE; Bleakman, D; Alt, A; Arnold, BM; Bell, MG; Bleisch, TJ; Castaņo, AM; Del Prado, M; Dominguez, E; Escribano, AM; Filla, SA; Ho, KH; Hudziak, KJ; Jones, CK; Mateo, A; Mathes, BM; Mattiuz, EL; Ogden, AM; Simmons, RM; Stack, DR; Stratford, RE; Winter, MA; Wu, Z; Ornstein, PL GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models. Bioorg Med Chem Lett23:6459-62 (2013) [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 |
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| 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 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 103984.96 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P39086 |
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| Residue: | 918 |
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| Sequence: | MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKF
AVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQ
SICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDS
TGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEIL
KQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSME
RLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRF
MNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGI
WNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCL
DLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREK
VIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFT
PYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTL
IIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKM
WAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYG
VGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFI
VLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECG
KLIREERGIRKQSSVHTV
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| BDBM50494060 |
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| n/a |
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| Name | BDBM50494060 |
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| Synonyms: | CHEMBL2440687 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H22ClNO5 |
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| Mol. Mass. | 355.813 |
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| SMILES | Cl.[H][C@@]12CC[C@@H](C[C@]1([H])C[C@H](NC2)C(O)=O)Oc1ccccc1C(O)=O |r| |
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| Structure | 
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