Reaction Details Report a problem with these data
Target
Metabotropic glutamate receptor 3
Ligand
BDBM50134449
Substrate
n/a
Meas. Tech.
ChEMBL_1544992 (CHEMBL3749857)
EC50
34±n/a nM
Citation
 Conde-Ceide, S; Alcázar, J; Alonso de Diego, SA; López, S; Martín-Martín, ML; Martínez-Viturro, CM; Pena, MA; Tong, HM; Lavreysen, H; Mackie, C; Bridges, TM; Daniels, JS; Niswender, CM; Jones, CK; Macdonald, GJ; Steckler, T; Conn, PJ; Stauffer, SR; Lindsley, CW; Bartolomé-Nebreda, JM Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. Bioorg Med Chem Lett 26:429-34 (2016) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 3
Synonyms:
GPRC1C | GRM3 | GRM3_HUMAN | MGLUR3 | metabotropic glutamate 3 | metabotropic glutamate 3/1a | metabotropic glutamate 3/1c
Type:
Enzyme Catalytic Domain
Mol. Mass.:
98889.09
Organism:
Homo sapiens (Human)
Description:
metabotropic glutamate 1c 0 HUMAN::Q14832
Residue:
879
Sequence:
MKMLTRLQVLTLALFSKGFLLSLGDHNFLRREIKIEGDLVLGGLFPINEKGTGTEECGRINEDRGIQRLEAMLFAIDEINKDDYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKVDEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNICIATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAASRANASFTWVASDGWGAQESIIKGSEHVAYGAITLELASQPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQCSLQNKRNHRRVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCDAMKILDGKKLYKDYLLKINFTAPFNPNKDADSIVKFDTFGDGMGRYNVFNFQNVGGKYSYLKVGHWAETLSLDVNSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYLADEFTCMDCGSGQWPTADLTGCYDLPEDYIRWEDAWAIGPVTIACLGFMCTCMVVTVFIKHNNTPLVKASGRELCYILLFGVGLSYCMTFFFIAKPSPVICALRRLGLGSSFAICYSALLTKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILEAPGTRRYTLAEKRETVILKCNVKDSSMLISLTYDVILVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIILFQPQKNVVTHRLHLNRFSVSGTGTTYSQSSASTYVPTVCNGREVLDSTTSSL
  
Inhibitor
Name:
BDBM50134449
Synonyms:
CHEMBL3745812
Type:
Small organic molecule
Emp. Form.:
C19H15F2N3O2
Mol. Mass.:
355.3381
SMILES:
Fc1ccc(OCc2cc3C(=O)N(CCn3n2)c2ccc(F)cc2)cc1
Structure:
Search PDB for entries with ligand similarity: