Assay Detail
Binding
CHEMBL3858844
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 7.48 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3901998 | — | — | 1 | 8.59 |
| CHEMBL3910866 | — | — | 1 | 8.01 |
| CHEMBL3947590 | — | — | 1 | 7.87 |
| CHEMBL3938796 | — | — | 1 | 7.82 |
| CHEMBL3919807 | — | — | 1 | 7.82 |
| CHEMBL3957311 | — | — | 1 | 7.77 |
| CHEMBL2179319 | — | — | 1 | 7.77 |
| CHEMBL3947764 | — | — | 1 | 7.68 |
| CHEMBL3985987 | — | — | 1 | 7.66 |
| CHEMBL3981882 | — | — | 1 | 7.58 |
| CHEMBL3928875 | — | — | 1 | 7.58 |
| CHEMBL3892865 | — | — | 1 | 7.42 |
| CHEMBL3956434 | — | — | 1 | 7.24 |
| CHEMBL3963034 | — | — | 1 | 7.24 |
| CHEMBL3929786 | — | — | 1 | 7.24 |
| CHEMBL3929950 | — | — | 1 | 7.19 |
| CHEMBL3926416 | — | — | 1 | 7.11 |
| CHEMBL3940264 | — | — | 1 | 7.08 |
| CHEMBL3919978 | — | — | 1 | 6.88 |
| CHEMBL3337527 | JNJ-40411813 | 2.0 | 1 | 6.83 |
| CHEMBL3937907 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3901998 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3910866 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3947590 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL3938796 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3919807 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3957311 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2179319 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3947764 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3985987 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3981882 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3928875 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3892865 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3956434 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3963034 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3929786 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3929950 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3926416 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3940264 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3919978 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3337527 | JNJ-40411813 | EC50 | = | 147.0 | nM | 6.83 |
| CHEMBL3937907 | — | EC50 | = | 195.0 | nM | 6.71 |