Target
Glutamate receptor ionotropic, kainate 1
Ligand
BDBM50178136
Substrate
n/a
Meas. Tech.
ChEMBL_429146 (CHEMBL904263)
Kd
402±n/a nM
Citation
 Dolman, NPMore, JCAlt, AKnauss, JLPentikäinen, OTGlasser, CRBleakman, DMayer, MLCollingridge, GLJane, 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:
BDBM50178136
Synonyms:
(S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)-pyrimidine-2,4-dione | (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrimidine-2,4-dione | (S)-2-((3-(2-amino-2-carboxyethyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)methyl)benzoic acid | CHEMBL372797 | UBP-302
Type:
Small organic molecule
Emp. Form.:
C15H15N3O6
Mol. Mass.:
333.2961
SMILES:
N[C@@H](Cn1ccc(=O)n(Cc2ccccc2C(O)=O)c1=O)C(O)=O
Structure:
Search PDB for entries with ligand similarity: