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Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50494055
Substrate
n/a
Meas. Tech.
ChEMBL_990076 (CHEMBL2443753)
Ki
500±n/a nM
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 Lett 23:6459-62 (2013) [PubMed]  Article 
Target
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:
MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKFAVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQSICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDSTGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEILKQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSMERLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRFMNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGIWNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCLDLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREKVIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFTPYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKMWAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYGVGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFIVLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECGKLIREERGIRKQSSVHTV
  
Inhibitor
Name:
BDBM50494055
Synonyms:
CHEMBL2440699
Type:
Small organic molecule
Emp. Form.:
C23H26ClNO5
Mol. Mass.:
431.909
SMILES:
Cl.[H][C@@]12CC[C@@H](C[C@]1([H])C[C@H](NC2)C(O)=O)Oc1cc(ccc1C(O)=O)-c1ccccc1 |r|
Structure:
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