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Assay Detail

CHEMBL719088

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 1 (CHEMBL4477)
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 10 4.57 4.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280563 1 4.64
CHEMBL143210 1 4.50
CHEMBL277475 1 -
CHEMBL140197 2 -
CHEMBL33567 1 -
CHEMBL143267 1 -
CHEMBL343994 1 -
CHEMBL334160 1 -
CHEMBL284193 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280563 EC50 = 23000.0 nM 4.64
CHEMBL143210 EC50 = 32000.0 nM 4.50
CHEMBL277475 EC50 > 500000.0 nM -
CHEMBL140197 EC50 > 100000.0 nM -
CHEMBL33567 EC50 > 100000.0 nM -
CHEMBL143267 EC50 > 100000.0 nM -
CHEMBL343994 EC50 > 100000.0 nM -
CHEMBL334160 EC50 > 100000.0 nM -
CHEMBL140197 EC50 > 100000.0 nM -
CHEMBL284193 EC50 > 100000.0 nM -