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Assay Detail

CHEMBL4023220

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Functional
Agonist activity at human mGlu2 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
20
Total Activities
20
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 2 (CHEMBL5137)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist.
Monn JA, Henry SS, Massey SM, Clawson DK, Chen Q, Diseroad BA, Bhardwaj RM, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang XS, Carter JH, Getman BG, Adragni K, Broad LM, Sanger HE, Ursu D, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL, Hao J.
J Med Chem (2018) 61 : 2303 -2328
PubMed 29350927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.48 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4091735 1 8.42
CHEMBL4070866 1 8.20
CHEMBL4095567 1 8.16
CHEMBL8759 EGLUMETAD 2.0 1 8.15
CHEMBL4068189 1 8.13
CHEMBL4071962 1 8.08
CHEMBL4061162 1 7.80
CHEMBL4090293 1 7.77
CHEMBL4091203 1 7.74
CHEMBL4063336 1 7.72
CHEMBL4095995 1 7.70
CHEMBL2381647 1 7.67
CHEMBL4099470 1 7.58
CHEMBL4098939 1 7.37
CHEMBL4081453 1 7.32
CHEMBL2381649 1 6.59
CHEMBL4068679 1 6.29
CHEMBL4069251 1 6.05
CHEMBL4060567 1 5.47
CHEMBL4093017 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4091735 EC50 = 3.77 nM 8.42
CHEMBL4070866 EC50 = 6.32 nM 8.20
CHEMBL4095567 EC50 = 6.97 nM 8.16
CHEMBL8759 EGLUMETAD EC50 = 7.0 nM 8.15
CHEMBL4068189 EC50 = 7.44 nM 8.13
CHEMBL4071962 EC50 = 8.37 nM 8.08
CHEMBL4061162 EC50 = 16.0 nM 7.80
CHEMBL4090293 EC50 = 17.1 nM 7.77
CHEMBL4091203 EC50 = 18.1 nM 7.74
CHEMBL4063336 EC50 = 19.1 nM 7.72
CHEMBL4095995 EC50 = 19.8 nM 7.70
CHEMBL2381647 EC50 = 21.2 nM 7.67
CHEMBL4099470 EC50 = 26.5 nM 7.58
CHEMBL4098939 EC50 = 42.5 nM 7.37
CHEMBL4081453 EC50 = 47.5 nM 7.32
CHEMBL2381649 EC50 = 257.0 nM 6.59
CHEMBL4068679 EC50 = 508.0 nM 6.29
CHEMBL4069251 EC50 = 893.0 nM 6.05
CHEMBL4060567 EC50 = 3390.0 nM 5.47
CHEMBL4093017 EC50 > 25000.0 nM -