Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM86751
Substrate
n/a
Meas. Tech.
ChEMBL_303286 (CHEMBL828279)
Ki
4160±n/a nM
Citation
 Dominguez, EIyengar, SShannon, HEBleakman, DAlt, AArnold, BMBell, MGBleisch, TJBuckmaster, JLCastano, AMDel Prado, MEscribano, AFilla, SAHo, KHHudziak, KJJones, CKMartinez-Perez, JAMateo, AMathes, BMMattiuz, ELOgden, AMSimmons, RMStack, DRStratford, REWinter, MAWu, ZOrnstein, PL Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. J Med Chem 48:4200-3 (2005) [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:
BDBM86751
Synonyms:
CHEMBL14935 | LY 293558 | LY-293558
Type:
Small organic molecule
Emp. Form.:
C13H21N5O2
Mol. Mass.:
279.3381
SMILES:
OC(=O)[C@@H]1C[C@H]2C[C@@H](CCc3nnn[nH]3)CC[C@H]2CN1
Structure:
Search PDB for entries with ligand similarity: