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Assay Detail

CHEMBL4037496

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Functional
Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 6 (CHEMBL4573)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
Selvam C, Lemasson IA, Brabet I, Oueslati N, Karaman B, Cabaye A, Tora AS, Commare B, Courtiol T, Cesarini S, McCort-Tranchepain I, Rigault D, Mony L, Bessiron T, McLean H, Leroux FR, Colobert F, Daniel H, Goupil-Lamy A, Bertrand HO, Goudet C, Pin JP, Acher FC.
J Med Chem (2018) 61 : 1969 -1989
PubMed 29397723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.10 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3114672 1 5.77
CHEMBL33567 1 5.62
CHEMBL4061423 1 5.44
CHEMBL4063142 1 5.24
CHEMBL4060360 1 5.22
CHEMBL4067923 1 5.21
CHEMBL4093492 1 5.06
CHEMBL285043 1 4.96
CHEMBL4091029 1 4.60
CHEMBL1089515 1 4.51
CHEMBL4095462 1 4.51
CHEMBL4061539 1 -
CHEMBL4101241 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3114672 EC50 = 1700.0 nM 5.77
CHEMBL33567 EC50 = 2400.0 nM 5.62
CHEMBL4061423 EC50 = 3600.0 nM 5.44
CHEMBL4063142 EC50 = 5700.0 nM 5.24
CHEMBL4060360 EC50 = 6000.0 nM 5.22
CHEMBL4067923 EC50 = 6100.0 nM 5.21
CHEMBL4093492 EC50 = 8800.0 nM 5.06
CHEMBL285043 EC50 = 11000.0 nM 4.96
CHEMBL4091029 EC50 = 25000.0 nM 4.60
CHEMBL1089515 EC50 = 31000.0 nM 4.51
CHEMBL4095462 EC50 = 31000.0 nM 4.51
CHEMBL4061539 EC50 > 100000.0 nM -
CHEMBL4101241 EC50 > 100000.0 nM -