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Target
Metabotropic glutamate receptor 1
Ligand
BDBM50231757
Substrate
n/a
Meas. Tech.
ChEMBL_460661 (CHEMBL926735)
IC50
110±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:
BDBM50231757
Synonyms:
2-[4-(4-fluoro-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydroquinoline-3-carbonitrile | CHEMBL401096
Type:
Small organic molecule
Emp. Form.:
C23H22FN3O
Mol. Mass.:
375.4387
SMILES:
CC1(C)CC(=O)c2cc(C#N)c(nc2C1)N1CCC(=CC1)c1ccc(F)cc1 |c:20|