Assay Detail
Binding
CHEMBL4023217
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Displacement of [3H]-LY459477 from recombinant human mGlu2 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.52 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4091735 | — | — | 1 | 7.50 |
| CHEMBL4070866 | — | — | 1 | 7.26 |
| CHEMBL4068189 | — | — | 1 | 7.24 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 7.14 |
| CHEMBL4071962 | — | — | 1 | 7.07 |
| CHEMBL4095567 | — | — | 1 | 6.86 |
| CHEMBL4099470 | — | — | 1 | 6.82 |
| CHEMBL4061162 | — | — | 1 | 6.73 |
| CHEMBL4091203 | — | — | 1 | 6.67 |
| CHEMBL4090293 | — | — | 1 | 6.66 |
| CHEMBL4095995 | — | — | 1 | 6.53 |
| CHEMBL4063336 | — | — | 1 | 6.48 |
| CHEMBL4098939 | — | — | 1 | 6.41 |
| CHEMBL4081453 | — | — | 1 | 6.38 |
| CHEMBL4069251 | — | — | 1 | 6.22 |
| CHEMBL4093017 | — | — | 1 | 6.20 |
| CHEMBL2381649 | — | — | 1 | 6.05 |
| CHEMBL4060567 | — | — | 1 | 5.82 |
| CHEMBL2381647 | — | — | 1 | 5.36 |
| CHEMBL4068679 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4091735 | — | Ki | = | 31.5 | nM | 7.50 |
| CHEMBL4070866 | — | Ki | = | 54.7 | nM | 7.26 |
| CHEMBL4068189 | — | Ki | = | 58.2 | nM | 7.24 |
| CHEMBL8759 | EGLUMETAD | Ki | = | 71.7 | nM | 7.14 |
| CHEMBL4071962 | — | Ki | = | 85.3 | nM | 7.07 |
| CHEMBL4095567 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL4099470 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL4061162 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL4091203 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL4090293 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4095995 | — | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL4063336 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL4098939 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL4081453 | — | Ki | = | 412.0 | nM | 6.38 |
| CHEMBL4069251 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL4093017 | — | Ki | = | 627.0 | nM | 6.20 |
| CHEMBL2381649 | — | Ki | = | 898.0 | nM | 6.05 |
| CHEMBL4060567 | — | Ki | = | 1520.0 | nM | 5.82 |
| CHEMBL2381647 | — | Ki | = | 4410.0 | nM | 5.36 |
| CHEMBL4068679 | — | Ki | = | 11200.0 | nM | 4.95 |