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Target
Metabotropic glutamate receptor 5
Ligand
BDBM44464
Substrate
n/a
Meas. Tech.
ChEMBL_887240 (CHEMBL2215796)
EC50
780±n/a nM
Citation
Rodriguez, AL; Zhou, Y; Williams, R; David Weaver, C; Vinson, PN; Dawson, ES; Steckler, T; Lavreysen, H; Mackie, C; Bartolomé, JM; Macdonald, GJ; Scott Daniels, J; Niswender, CM; Jones, CK; Jeffrey Conn, P; Lindsley, CW; Stauffer, SR Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold. Bioorg Med Chem Lett 22:7388-92 (2012) [PubMed] Article
More Info.:
Target
Name:
Metabotropic glutamate receptor 5
Synonyms:
GPRC1E | GRM5 | GRM5_HUMAN | MGLUR5 | metabotropic glutamate 5 | metabotropic glutamate 5a
Type:
Enzyme
Mol. Mass.:
132484.72
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
1212
Sequence:
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQHRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPGYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVVFIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTSTVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGNGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRGLGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPSPISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAARESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSSSSL
Inhibitor
Name:
BDBM44464
Synonyms:
2-(2-chloro-N-mesyl-anilino)-N-(3-chlorophenyl)acetamide | 2-(2-chloro-N-methylsulfonylanilino)-N-(3-chlorophenyl)acetamide | CHEMBL1451902 | MLS000530551 | N-(3-chlorophenyl)-2-[(2-chlorophenyl)-methylsulfonyl-amino]ethanamide | N~2~-(2-chlorophenyl)-N~1~-(3-chlorophenyl)-N~2~-(methylsulfonyl)glycinamide | SMR000135531 | cid_1364364
Type:
Small organic molecule
Emp. Form.:
C15H14Cl2N2O3S
Mol. Mass.:
373.254
SMILES:
CS(=O)(=O)N(CC(=O)Nc1cccc(Cl)c1)c1ccccc1Cl