Reaction Details Report a problem with these data
Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50002369
Substrate
n/a
Meas. Tech.
ChEMBL_573958 (CHEMBL1062119)
EC50
37000±n/a nM
Citation
 Clausen, RP; Naur, P; Kristensen, AS; Greenwood, JR; Strange, M; Bräuner-Osborne, H; Jensen, AA; Nielsen, AS; Geneser, U; Ringgaard, LM; Nielsen, B; Pickering, DS; Brehm, L; Gajhede, M; Krogsgaard-Larsen, P; Kastrup, JS The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization. J Med Chem 52:4911-22 (2009) [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:
BDBM50002369
Synonyms:
(2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid | (3S,4R)-3-(carboxymethyl)-4-(prop-1-en-2-yl)-L-proline | CHEMBL275040 | Digenin | Digensaeure | Helminal | Kainate | Kainsaeure | L-alpha-kainic acid | alpha-Kainic acid | digenic acid | kainic acid
Type:
Small organic molecule
Emp. Form.:
C10H15NO4
Mol. Mass.:
213.2304
SMILES:
CC(=C)[C@H]1CN[C@@H]([C@H]1CC(O)=O)C(O)=O |r|
Structure:
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