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Target
Metabotropic glutamate receptor 1
Ligand
BDBM50231732
Substrate
n/a
Meas. Tech.
ChEMBL_460664 (CHEMBL926738)
IC50
12000±n/a nM
Citation
Vanejevs, M; Jatzke, C; Renner, S; Müller, S; Hechenberger, M; Bauer, T; Klochkova, A; Pyatkin, I; Kazyulkin, D; Aksenova, E; Shulepin, S; Timonina, O; Haasis, A; Gutcaits, A; Parsons, CG; Kauss, V; Weil, T Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem 51:634-47 (2008) [PubMed] Article
More Info.:
Target
Name:
Metabotropic glutamate receptor 1
Synonyms:
GRM1_RAT | Gprc1a | Grm1 | Metabotropic Glutamate 1a | Metabotropic glutamate receptor | Metabotropic glutamate receptor 1 | Mglur1 | metabotropic glutamate 1 | metabotropic glutamate 1/5-D | metabotropic glutamate 1/DA | metabotropic glutamate receptor 1 isoform alpha precursor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
133240.47
Organism:
RAT
Description:
metabotropic glutamate 1/2 0 RAT::P23385
Residue:
1199
Sequence:
MVRLLLIFFPMIFLEMSILPRMPDRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGLNRCLPDGQTLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKKVCTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGRKLLDFLIKSSFVGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGMVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEFVQDEFTCRACDLGWWPNAELTGCEPIPVRYLEWSDIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPVGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKPGAGNANSNGKSVSWSEPGGRQAPKGQHVWQRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDASTKTLYNVEEEDNTPSAHFSPPSSPSMVVHRRGPPVATTPPLPPHLTAEETPLFLADSVIPKGLPPPLPQQQPQQPPPQQPPQQPKSLMDQLQGVVTNFGSGIPDFHAVLAGPGTPGNSLRSLYPPPPPPQHLQMLPLHLSTFQEESISPPGEDIDDDSERFKLLQEFVYEREGNTEEDELEEEEDLPTASKLTPEDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVTYASVILRDYKQSSSTL
Inhibitor
Name:
BDBM50231732
Synonyms:
7,7-dimethyl-3-nitro-2-(4-phenyl-3,6-dihydro-2H-pyridin-1-yl)-7,8-dihydro-6H-quinolin-5-one | CHEMBL252543
Type:
Small organic molecule
Emp. Form.:
C23H24FN3O3
Mol. Mass.:
409.4534
SMILES:
CC1(C)CC(=O)c2cc(c(NC3CCC(=CC3)c3ccc(F)cc3)nc2C1)[N+]([O-])=O |w:11.10,c:14|