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Target
Metabotropic glutamate receptor 5
Ligand
BDBM50395923
Substrate
n/a
Meas. Tech.
ChEMBL_858340 (CHEMBL2168339)
Kd
9.4±n/a nM
Citation
 Raboisson, P; Breitholtz-Emanuelsson, A; Dahllöf, H; Edwards, L; Heaton, WL; Isaac, M; Jarvie, K; Kers, A; Minidis, AB; Nordmark, A; Sheehan, SM; Slassi, A; Ström, P; Terelius, Y; Wensbo, D; Wilson, JM; Xin, T; McLeod, DA Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett 22:6974-9 (2012) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 5
Synonyms:
GRM5_RAT | Gprc1e | Grm5 | Metabotropic glutamate receptor | Mglur5 | metabotropic glutamate 5 | metabotropic glutamate 5/1-C | metabotropic glutamate 5/1-F | metabotropic glutamate 5a
Type:
Enzyme
Mol. Mass.:
131900.14
Organism:
Rattus norvegicus (Rat)
Description:
P31424
Residue:
1203
Sequence:
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLRSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNLRNPWFQEFWQHRFQCRLEGFAQENSKYNKTCNSSLTLRTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCPGYAGLCDAMKPIDGRKLLDSLMKTNFTGVSGDMILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNGELKMDDDEVWSKKNNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVIFIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTSTVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGNGGRATMSSSNGKSVTWAQNEKSTRGQHLWQRLSVHINKKENPNQTAVIKPFPKSTENRGPGAAAGGGSGPGVAGAGNAGCTATGGPEPPDAGPKALYDVAEAEESFPAAARPRSPSPISTLSHLAGSAGRTDDDAPSLHSETAARSSSSQGSLMEQISSVVTRFTANISELNSMMLSTAATPGPPGTPICSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQGATGVSPAQETPTGAESAPGKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTLIIRDYTQSSSSL
  
Inhibitor
Name:
BDBM50395923
Synonyms:
CHEMBL2164550
Type:
Small organic molecule
Emp. Form.:
C14H6F2N4O
Mol. Mass.:
284.2204
SMILES:
Fc1ccc(nc1)-c1noc(n1)-c1cc(F)cc(c1)C#N
Structure:
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