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Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50399431
Substrate
n/a
Meas. Tech.
ChEMBL_878019 (CHEMBL2182445)
IC50
0.82±n/a nM
Citation
 Lucas, S; Poulsen, MH; Nørager, NG; Barslund, AF; Bach, TB; Kristensen, AS; Strømgaard, K General synthesis ofß-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors. J Med Chem 55:10297-301 (2012) [PubMed]  Article 
Target
Name:
Glutamate receptor ionotropic, kainate 1
Synonyms:
GRIK1_RAT | Glur5 | Glutamate receptor ionotropic kainate 1 | Glutamate receptor ionotropic, kainate | Glutamate receptor, ionotropic kainate 1 | Glutamate-Kainate | Grik1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
107860.82
Organism:
RAT
Description:
P22756
Residue:
949
Sequence:
MERSTVLIQPGLWTRDTSWTLLYFLCYILPQTSPQVLRIGGIFETVENEPVNVEELAFKFAVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQSICNALEVPHIQTRWKHPSVDSRDLFYINLYPDYAAISRAVLDLVLYYNWKTVTVVYEDSTGLIRLQELIKAPSRYNIKIKIRQLPPANKDAKPLLKEMKKSKEFYVIFDCSHETAAEILKQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRKLNIDNPHVSSIIEKWSMERLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPCALGPRFMNLIKEARWDGLTGRITFNKTDGLRKDFDLDIISLKEEGTEKASGEVSKHLYKVWKKIGIWNSNSGLNMTDGNRDRSNNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEAYCLDLLKELSNILGFLYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREKVIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFTPYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTLIIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKMWAFMSSRQQSALVKNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYGVGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDSKEASALGVENIGGIFIVLAAGLVLSVFVAIGEFLYKSRKNNDVEQKGKSSRLRFYFRNKVRFHGSKKESLGVEKCLSFNAIMEELGISLKNQKKLKKKSRTKGKSSFTSILTCHQRRTQRKETVA
  
Inhibitor
Name:
BDBM50399431
Synonyms:
CHEMBL2178919
Type:
Small organic molecule
Emp. Form.:
C29H48N8O4
Mol. Mass.:
572.7426
SMILES:
NCCCNCCCCNCCC(=O)NCCCCCNC(=O)[C@H](CC(N)=O)NC(=O)Cc1c[nH]c2ccccc12 |r|
Structure:
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