Reaction Details Report a problem with these data
Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50126763
Substrate
n/a
Meas. Tech.
ChEMBL_573947 (CHEMBL1059439)
Ki
2.13±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
More Info.:
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:
BDBM50126763
Synonyms:
(S)-2-amino-3-(3-hydroxy-5-tert-butyl-4-isoxazolyl)propionic acid | 2-Amino-3-(5-tert-butyl-3-hydroxy-isoxazol-4-yl)-propionic acid | CHEMBL27130
Type:
Small organic molecule
Emp. Form.:
C10H16N2O4
Mol. Mass.:
228.245
SMILES:
CC(C)(C)c1o[nH]c(=O)c1C[C@H](N)C(O)=O