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Assay Detail

CHEMBL872629

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Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type neuronal
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 8 (CHEMBL2718)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.
Collado I, Pedregal C, Bueno AB, Marcos A, González R, Blanco-Urgoiti J, Pérez-Castells J, Schoepp DD, Wright RA, Johnson BG, Kingston AE, Moher ED, Hoard DW, Griffey KI, Tizzano JP.
J Med Chem (2004) 47 : 456 -466
PubMed 14711315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.95 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140197 1 8.00
CHEMBL143210 1 7.51
CHEMBL33567 1 7.22
CHEMBL277475 1 6.68
CHEMBL280563 1 6.40
CHEMBL334160 1 5.88
CHEMBL357043 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140197 EC50 = 10.0 nM 8.00
CHEMBL143210 EC50 = 31.0 nM 7.51
CHEMBL33567 EC50 = 60.0 nM 7.22
CHEMBL277475 EC50 = 210.0 nM 6.68
CHEMBL280563 EC50 = 400.0 nM 6.40
CHEMBL334160 EC50 = 1320.0 nM 5.88
CHEMBL357043 EC50 > 100000.0 nM -