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Target
Metabotropic glutamate receptor 1
Ligand
BDBM50094841
Substrate
n/a
Meas. Tech.
ChEMBL_2053747 (CHEMBL4708748)
IC50
>30000±n/a nM
Citation
 Urabe, H; Miyakoshi, N; Ohtake, N; Nozoe, A; Ochi, M; Fukasawa, M; Kinoshita, K; Yamaguchi, JI; Marumo, T; Hikichi, H; Chaki, S; Hashihayata, T Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability. Eur J Med Chem 203:0 (2020) [PubMed]  Article
Target
Name:
Metabotropic glutamate receptor 1
Synonyms:
GPRC1A | GRM1 | GRM1_HUMAN | MGLUR1 | Metabotropic Glutamate 1a | metabotropic glutamate 1
Type:
Enzyme
Mol. Mass.:
132358.19
Organism:
Homo sapiens (Human)
Description:
Q13255
Residue:
1194
Sequence:
MVGLLLFFFPAIFLEVSLLPRSPGRKVLLAGASSQRSVARMDGDVIIGALFSVHHQPPAEKVPERKCGEIREQYGIQRVEAMFHTLDKINADPVLLPNITLGSEIRDSCWHSSVALEQSIEFIRDSLISIRDEKDGINRCLPDGQSLPPGRTKKPIAGVIGPGSSSVAIQVQNLLQLFDIPQIAYSATSIDLSDKTLYKYFLRVVPSDTLQARAMLDIVKRYNWTYVSAVHTEGNYGESGMDAFKELAAQEGLCIAHSDKIYSNAGEKSFDRLLRKLRERLPKARVVVCFCEGMTVRGLLSAMRRLGVVGEFSLIGSDGWADRDEVIEGYEVEANGGITIKLQSPEVRSFDDYFLKLRLDTNTRNPWFPEFWQHRFQCRLPGHLLENPNFKRICTGNESLEENYVQDSKMGFVINAIYAMAHGLQNMHHALCPGHVGLCDAMKPIDGSKLLDFLIKSSFIGVSGEEVWFDEKGDAPGRYDIMNLQYTEANRYDYVHVGTWHEGVLNIDDYKIQMNKSGVVRSVCSEPCLKGQIKVIRKGEVSCCWICTACKENEYVQDEFTCKACDLGWWPNADLTGCEPIPVRYLEWSNIESIIAIAFSCLGILVTLFVTLIFVLYRDTPVVKSSSRELCYIILAGIFLGYVCPFTLIAKPTTTSCYLQRLLVGLSSAMCYSALVTKTNRIARILAGSKKKICTRKPRFMSAWAQVIIASILISVQLTLVVTLIIMEPPMPILSYPSIKEVYLICNTSNLGVVAPLGYNGLLIMSCTYYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITTCFAVSLSVTVALGCMFTPKMYIIIAKPERNVRSAFTTSDVVRMHVGDGKLPCRSNTFLNIFRRKKAGAGNANSNGKSVSWSEPGGGQVPKGQHMWHRLSVHVKTNETACNQTAVIKPLTKSYQGSGKSLTFSDTSTKTLYNVEEEEDAQPIRFSPPGSPSMVVHRRVPSAATTPPLPSHLTAEETPLFLAEPALPKGLPPPLQQQQQPPPQQKSLMDQLQGVVSNFSTAIPDFHAVLAGPGGPGNGLRSLYPPPPPPQHLQMLPLQLSTFGEELVSPPADDDDDSERFKLLQEYVYEHEREGNTEEDELEEEEEDLQAASKLTPDDSPALTPPSPFRDSVASGSSVPSSPVSESVLCTPPNVSYASVILRDYKQSSSTL
  
Inhibitor
Name:
BDBM50094841
Synonyms:
(+)-2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid | (-)-2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid | (1S,2S,3S,5R,6S)-2-amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid | 2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid | CHEMBL334014
Type:
Small organic molecule
Emp. Form.:
C8H10FNO4
Mol. Mass.:
203.1677
SMILES:
N[C@@]1([C@H]2[C@@H](C[C@@H]1F)[C@@H]2C(O)=O)C(O)=O
Structure:
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