Assay Detail
Functional
CHEMBL3876529
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Positive allosteric modulation of human mGlu2 receptor expressed in HEK293 cells coexpressing rat glutamate transporter assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins in presence of orthosteric antagonist LY341495 by FLIPR assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 8.02 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3883435 | — | — | 1 | 9.40 |
| CHEMBL3884532 | — | — | 1 | 9.40 |
| CHEMBL3884187 | — | — | 1 | 9.30 |
| CHEMBL3884636 | — | — | 1 | 8.89 |
| CHEMBL3885379 | — | — | 1 | 8.85 |
| CHEMBL3883634 | — | — | 1 | 8.77 |
| CHEMBL3884094 | — | — | 1 | 8.74 |
| CHEMBL3884833 | — | — | 1 | 8.40 |
| CHEMBL3884936 | — | — | 1 | 8.26 |
| CHEMBL3885115 | — | — | 1 | 8.21 |
| CHEMBL3883801 | — | — | 1 | 8.17 |
| CHEMBL3884343 | — | — | 1 | 8.00 |
| CHEMBL3884075 | — | — | 1 | 7.96 |
| CHEMBL3884332 | — | — | 1 | 7.96 |
| CHEMBL3885396 | — | — | 1 | 7.89 |
| CHEMBL3885312 | — | — | 1 | 7.89 |
| CHEMBL3885265 | — | — | 1 | 7.80 |
| CHEMBL3885097 | — | — | 1 | 7.77 |
| CHEMBL3885072 | — | — | 1 | 7.75 |
| CHEMBL3885277 | — | — | 1 | 7.70 |
| CHEMBL3885353 | — | — | 1 | 7.55 |
| CHEMBL3883585 | — | — | 1 | 7.54 |
| CHEMBL3883827 | — | — | 1 | 7.50 |
| CHEMBL3884170 | — | — | 1 | 7.22 |
| CHEMBL3885492 | — | — | 1 | 6.75 |
| CHEMBL3885493 | — | — | 1 | 6.64 |
| CHEMBL3884042 | — | — | 1 | 6.14 |
| CHEMBL3883462 | — | — | 1 | - |
| CHEMBL3883487 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3883435 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3884532 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3884187 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3884636 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3885379 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3883634 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3884094 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3884833 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3884936 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3885115 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3883801 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3884343 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3884075 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3884332 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3885396 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3885312 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3885265 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3885097 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3885072 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3885277 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3885353 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3883585 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3883827 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3884170 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3885492 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3885493 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3884042 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3883462 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3883487 | — | EC50 | > | 15000.0 | nM | - |