Assay Detail
Binding
CHEMBL4023218
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LY459477 from recombinant human mGlu3 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 | 7.73 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071962 | — | — | 1 | 9.33 |
| CHEMBL4081453 | — | — | 1 | 9.03 |
| CHEMBL4068189 | — | — | 1 | 8.75 |
| CHEMBL4091203 | — | — | 1 | 8.68 |
| CHEMBL4091735 | — | — | 1 | 8.64 |
| CHEMBL4095567 | — | — | 1 | 8.64 |
| CHEMBL4063336 | — | — | 1 | 8.36 |
| CHEMBL4061162 | — | — | 1 | 8.34 |
| CHEMBL4090293 | — | — | 1 | 8.24 |
| CHEMBL4095995 | — | — | 1 | 8.17 |
| CHEMBL4070866 | — | — | 1 | 8.03 |
| CHEMBL4099470 | — | — | 1 | 7.63 |
| CHEMBL4098939 | — | — | 1 | 7.56 |
| CHEMBL8759 | EGLUMETAD | 2.0 | 1 | 6.97 |
| CHEMBL2381649 | — | — | 1 | 6.75 |
| CHEMBL4069251 | — | — | 1 | 6.55 |
| CHEMBL2381647 | — | — | 1 | 6.55 |
| CHEMBL4093017 | — | — | 1 | 6.37 |
| CHEMBL4060567 | — | — | 1 | 6.12 |
| CHEMBL4068679 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071962 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL4081453 | — | Ki | = | 0.927 | nM | 9.03 |
| CHEMBL4068189 | — | Ki | = | 1.79 | nM | 8.75 |
| CHEMBL4091203 | — | Ki | = | 2.11 | nM | 8.68 |
| CHEMBL4091735 | — | Ki | = | 2.27 | nM | 8.64 |
| CHEMBL4095567 | — | Ki | = | 2.29 | nM | 8.64 |
| CHEMBL4063336 | — | Ki | = | 4.34 | nM | 8.36 |
| CHEMBL4061162 | — | Ki | = | 4.56 | nM | 8.34 |
| CHEMBL4090293 | — | Ki | = | 5.79 | nM | 8.24 |
| CHEMBL4095995 | — | Ki | = | 6.75 | nM | 8.17 |
| CHEMBL4070866 | — | Ki | = | 9.34 | nM | 8.03 |
| CHEMBL4099470 | — | Ki | = | 23.2 | nM | 7.63 |
| CHEMBL4098939 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL8759 | EGLUMETAD | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL2381649 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL4069251 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL2381647 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL4093017 | — | Ki | = | 425.0 | nM | 6.37 |
| CHEMBL4060567 | — | Ki | = | 757.0 | nM | 6.12 |
| CHEMBL4068679 | — | Ki | = | 1070.0 | nM | 5.97 |