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Target
Metabotropic glutamate receptor 3
Ligand
BDBM50558766
Substrate
n/a
Meas. Tech.
ChEMBL_2064698 (CHEMBL4719951)
IC50
2.5±n/a nM
Citation
 Chappell, MD; Li, R; Smith, SC; Dressman, BA; Tromiczak, EG; Tripp, AE; Blanco, MJ; Vetman, T; Quimby, SJ; Matt, J; Britton, TC; Fivush, AM; Schkeryantz, JM; Mayhugh, D; Erickson, JA; Bures, MG; Jaramillo, C; Carpintero, M; Diego, JE; Barberis, M; Garcia-Cerrada, S; Soriano, JF; Antonysamy, S; Atwell, S; MacEwan, I; Condon, B; Sougias, C; Wang, J; Zhang, A; Conners, K; Groshong, C; Wasserman, SR; Koss, JW; Witkin, JM; Li, X; Overshiner, C; Wafford, KA; Seidel, W; Wang, XS; Heinz, BA; Swanson, S; Catlow, JT; Bedwell, DW; Monn, JA; Mitch, CH; Ornstein, PL Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity. J Med Chem 59:10974-10993 (2016) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 3
Synonyms:
metabotropic glutamate 3 | metabotropic glutamate 3/1a | metabotropic glutamate 3/1c | GRM3_HUMAN | GRM3 | GPRC1C | MGLUR3
Type:
Enzyme Catalytic Domain
Mol. Mass.:
98889.09
Organism:
Human
Description:
metabotropic glutamate 1c 0 HUMAN::Q14832
Residue:
879
Sequence:
MKMLTRLQVLTLALFSKGFLLSLGDHNFLRREIKIEGDLVLGGLFPINEKGTGTEECGRINEDRGIQRLEAMLFAIDEINKDDYLLPGVKLGVHILDTCSRDTYALEQSLEFVRASLTKVDEAEYMCPDGSYAIQENIPLLIAGVIGGSYSSVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFYQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFEQEARLRNICIATAEKVGRSNIRKSYDSVIRELLQKPNARVVVLFMRSDDSRELIAAASRANASFTWVASDGWGAQESIIKGSEHVAYGAITLELASQPVRQFDRYFQSLNPYNNHRNPWFRDFWEQKFQCSLQNKRNHRRVCDKHLAIDSSNYEQESKIMFVVNAVYAMAHALHKMQRTLCPNTTKLCDAMKILDGKKLYKDYLLKINFTAPFNPNKDADSIVKFDTFGDGMGRYNVFNFQNVGGKYSYLKVGHWAETLSLDVNSIHWSRNSVPTSQCSDPCAPNEMKNMQPGDVCCWICIPCEPYEYLADEFTCMDCGSGQWPTADLTGCYDLPEDYIRWEDAWAIGPVTIACLGFMCTCMVVTVFIKHNNTPLVKASGRELCYILLFGVGLSYCMTFFFIAKPSPVICALRRLGLGSSFAICYSALLTKTNCIARIFDGVKNGAQRPKFISPSSQVFICLGLILVQIVMVSVWLILEAPGTRRYTLAEKRETVILKCNVKDSSMLISLTYDVILVILCTVYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCISVSLSGFVVLGCLFAPKVHIILFQPQKNVVTHRLHLNRFSVSGTGTTYSQSSASTYVPTVCNGREVLDSTTSSL
  
Inhibitor
Name:
BDBM50558766
Synonyms:
CHEMBL4751065
Type:
Small organic molecule
Emp. Form.:
C15H16ClF2NO5S
Mol. Mass.:
395.81
SMILES:
c1cc(c(cc1SC[C@@H]2[C@H]([C@H]3[C@@H]([C@H]3[C@@]2(C(=O)O)N)C(=O)O)O)F)F
Structure:
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