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Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50207593
Substrate
n/a
Meas. Tech.
ChEMBL_429146 (CHEMBL904263)
Kd
18±n/a nM
Citation
 Dolman, NP; More, JC; Alt, A; Knauss, JL; Pentikäinen, OT; Glasser, CR; Bleakman, D; Mayer, ML; Collingridge, GL; Jane, DE Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. J Med Chem 50:1558-70 (2007) [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:
BDBM50207593
Synonyms:
(S)-1-(2-AMINO-2-CARBOXYETHYL)-3(2-CARBOXYTHIOPHENE-3-YL-METHYL)-5-METHYLPYRIMIDINE-2,4-DIONE | (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxythiophene-3-ylmethyl)-5-methylpyrimidine-2,4-dione | CHEMBL373428
Type:
Small organic molecule
Emp. Form.:
C14H15N3O6S
Mol. Mass.:
353.35
SMILES:
Cc1cn(C[C@H](N)C(O)=O)c(=O)n(Cc2ccsc2C(O)=O)c1=O
Structure:
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