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Target
Metabotropic glutamate receptor 1
Ligand
BDBM50214088
Substrate
n/a
Meas. Tech.
ChEMBL_456241 (CHEMBL888251)
IC50
180±n/a nM
Citation
 Wang, X; Kolasa, T; El Kouhen, OF; Chovan, LE; Black-Shaefer, CL; Wagenaar, FL; Garton, JA; Moreland, RB; Honore, P; Lau, YY; Dandliker, PJ; Brioni, JD; Stewart, AO Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett 17:4303-7 (2007) [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:
BDBM50214088
Synonyms:
5-(4-chlorophenyl)-6-methyl-1-m-tolyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one | CHEMBL400307
Type:
Small organic molecule
Emp. Form.:
C19H15ClN4O
Mol. Mass.:
350.802
SMILES:
Cc1cccc(c1)-n1ncc2c1nc(C)n(-c1ccc(Cl)cc1)c2=O
Structure:
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