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Target
Metabotropic glutamate receptor 4
Ligand
BDBM55091
Substrate
n/a
Meas. Tech.
ChEMBL_788856 (CHEMBL1924926)
EC50
435±n/a nM
Citation
Jones, CK; Engers, DW; Thompson, AD; Field, JR; Blobaum, AL; Lindsley, SR; Zhou, Y; Gogliotti, RD; Jadhav, S; Zamorano, R; Bogenpohl, J; Smith, Y; Morrison, R; Daniels, JS; Weaver, CD; Conn, PJ; Lindsley, CW; Niswender, CM; Hopkins, CR Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkin J Med Chem 54:7639-47 (2011) [PubMed] Article
More Info.:
Target
Name:
Metabotropic glutamate receptor 4
Synonyms:
GPRC1D | GRM4 | GRM4_HUMAN | Glutamate receptor, metabotropic 4 | MGLUR4 | Metabotropic glutamate receptor 4 | Metabotropic glutamate receptor 4 (mGlu4) | Metabotropic glutamate receptor 4 (mGluR4) | metabotropic glutamate 4
Type:
Protein
Mol. Mass.:
101899.95
Organism:
Homo sapiens (Human)
Description:
Q14833
Residue:
912
Sequence:
MPGKRGLGWWWARLPLCLLLSLYGPWMPSSLGKPKGHPHMNSIRIDGDITLGGLFPVHGRGSEGKPCGELKKEKGIHRLEAMLFALDRINNDPDLLPNITLGARILDTCSRDTHALEQSLTFVQALIEKDGTEVRCGSGGPPIITKPERVVGVIGASGSSVSIMVANILRLFKIPQISYASTAPDLSDNSRYDFFSRVVPSDTYQAQAMVDIVRALKWNYVSTVASEGSYGESGVEAFIQKSREDGGVCIAQSVKIPREPKAGEFDKIIRRLLETSNARAVIIFANEDDIRRVLEAARRANQTGHFFWMGSDSWGSKIAPVLHLEEVAEGAVTILPKRMSVRGFDRYFSSRTLDNNRRNIWFAEFWEDNFHCKLSRHALKKGSHVKKCTNRERIGQDSAYEQEGKVQFVIDAVYAMGHALHAMHRDLCPGRVGLCPRMDPVDGTQLLKYIRNVNFSGIAGNPVTFNENGDAPGRYDIYQYQLRNDSAEYKVIGSWTDHLHLRIERMHWPGSGQQLPRSICSLPCQPGERKKTVKGMPCCWHCEPCTGYQYQVDRYTCKTCPYDMRPTENRTGCRPIPIIKLEWGSPWAVLPLFLAVVGIAATLFVVITFVRYNDTPIVKASGRELSYVLLAGIFLCYATTFLMIAEPDLGTCSLRRIFLGLGMSISYAALLTKTNRIYRIFEQGKRSVSAPRFISPASQLAITFSLISLQLLGICVWFVVDPSHSVVDFQDQRTLDPRFARGVLKCDISDLSLICLLGYSMLLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIVWLAFIPIFFGTSQSADKLYIQTTTLTVSVSLSASVSLGMLYMPKVYIILFHPEQNVPKRKRSLKAVVTAATMSNKFTQKGNFRPNGEAKSELCENLEAPALATKQTYVTYTNHAI
Inhibitor
Name:
BDBM55091
Synonyms:
N-[3-chloranyl-4-[(1S,5R)-6,6-dimethyl-2,4-bis(oxidanylidene)-3-azabicyclo[3.1.0]hexan-3-yl]phenyl]pyridine-2-carboxamide | N-[3-chloro-4-[(1S,5R)-2,4-diketo-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-3-yl]phenyl]picolinamide | N-[3-chloro-4-[(1S,5R)-6,6-dimethyl-2,4-dioxo-3-azabicyclo[3.1.0]hexan-3-yl]phenyl]-2-pyridinecarboxamide | N-[3-chloro-4-[(1S,5R)-6,6-dimethyl-2,4-dioxo-3-azabicyclo[3.1.0]hexan-3-yl]phenyl]pyridine-2-carboxamide | VU0410425-1 | cid_46869949
Type:
Small organic molecule
Emp. Form.:
C19H16ClN3O3
Mol. Mass.:
369.802
SMILES:
CC1(C)c2c1c(O)n(c2O)-c1ccc(NC(=O)c2ccccn2)cc1Cl |(19.1,-1.33,;18.33,,;19.1,1.33,;17,.77,;17,-.77,;15.54,-1.25,;15.06,-2.71,;14.63,,;15.54,1.25,;15.06,2.71,;13.09,,;12.32,-1.33,;10.78,-1.33,;10.01,,;8.47,,;7.7,-1.33,;8.47,-2.67,;6.16,-1.33,;5.39,,;3.85,,;3.08,-1.33,;3.85,-2.67,;5.39,-2.67,;10.78,1.33,;12.32,1.33,;13.09,2.67,)|