Assay Detail
Functional
CHEMBL900011
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.29 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL238346 | — | — | 1 | 8.21 |
| CHEMBL235398 | — | — | 1 | 7.35 |
| CHEMBL237906 | — | — | 1 | 7.32 |
| CHEMBL397618 | — | — | 1 | 7.29 |
| CHEMBL397617 | — | — | 1 | 7.26 |
| CHEMBL391755 | — | — | 1 | 7.17 |
| CHEMBL395122 | — | — | 1 | 7.17 |
| CHEMBL235397 | — | — | 1 | 6.94 |
| CHEMBL397551 | — | — | 1 | 6.75 |
| CHEMBL235838 | — | — | 1 | 6.74 |
| CHEMBL395902 | — | — | 1 | 6.65 |
| CHEMBL235629 | — | — | 1 | 6.56 |
| CHEMBL238344 | — | — | 1 | 6.46 |
| CHEMBL238391 | — | — | 1 | 6.33 |
| CHEMBL235837 | — | — | 1 | 6.32 |
| CHEMBL97344 | — | — | 1 | 6.18 |
| CHEMBL236431 | — | — | 1 | 6.17 |
| CHEMBL238388 | — | — | 1 | 5.90 |
| CHEMBL238390 | — | — | 1 | 5.80 |
| CHEMBL235396 | — | — | 1 | 5.74 |
| CHEMBL392007 | — | — | 1 | 5.53 |
| CHEMBL236262 | — | — | 1 | 5.22 |
| CHEMBL238389 | — | — | 1 | 5.18 |
| CHEMBL238139 | — | — | 1 | 5.10 |
| CHEMBL236264 | — | — | 1 | 4.92 |
| CHEMBL236263 | — | — | 1 | 4.80 |
| CHEMBL394718 | — | — | 1 | 4.73 |
| CHEMBL235399 | — | — | 1 | - |
| CHEMBL236429 | — | — | 1 | - |
| CHEMBL235836 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL238346 | — | IC50 | = | 6.19 | nM | 8.21 |
| CHEMBL235398 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL237906 | — | IC50 | = | 47.9 | nM | 7.32 |
| CHEMBL397618 | — | IC50 | = | 51.7 | nM | 7.29 |
| CHEMBL397617 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL391755 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL395122 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL235397 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL397551 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL235838 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL395902 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL235629 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL238344 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL238391 | — | IC50 | = | 468.0 | nM | 6.33 |
| CHEMBL235837 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL97344 | — | IC50 | = | 664.0 | nM | 6.18 |
| CHEMBL236431 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL238388 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL238390 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL235396 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL392007 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL236262 | — | IC50 | = | 6070.0 | nM | 5.22 |
| CHEMBL238389 | — | IC50 | = | 6570.0 | nM | 5.18 |
| CHEMBL238139 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL236264 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL236263 | — | IC50 | = | 15700.0 | nM | 4.80 |
| CHEMBL394718 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL235399 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL236429 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL235836 | — | IC50 | > | 30000.0 | nM | - |