Assay Detail
Binding
CHEMBL1004108
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Displacement of [3H]MPEP from cloned mGluR5 expressed in HEK293T cells by scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK-293T |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.27 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446543 | — | — | 1 | 9.05 |
| CHEMBL511603 | — | — | 1 | 8.57 |
| CHEMBL184995 | — | — | 1 | 8.26 |
| CHEMBL369310 | — | — | 1 | 8.25 |
| CHEMBL466006 | — | — | 1 | 8.01 |
| CHEMBL365403 | — | — | 1 | 7.97 |
| CHEMBL443979 | — | — | 1 | 7.94 |
| CHEMBL66654 | — | — | 1 | 7.89 |
| CHEMBL493568 | — | — | 1 | 7.66 |
| CHEMBL468525 | — | — | 1 | 5.48 |
| CHEMBL501020 | — | — | 1 | 5.16 |
| CHEMBL493776 | — | — | 1 | 5.14 |
| CHEMBL468526 | — | — | 1 | 5.12 |
| CHEMBL493775 | — | — | 1 | - |
| CHEMBL464550 | — | — | 1 | - |
| CHEMBL512634 | — | — | 1 | - |
| CHEMBL493777 | — | — | 1 | - |
| CHEMBL493571 | — | — | 1 | - |
| CHEMBL292065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446543 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL511603 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL184995 | — | Ki | = | 5.49 | nM | 8.26 |
| CHEMBL369310 | — | Ki | = | 5.65 | nM | 8.25 |
| CHEMBL466006 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL365403 | — | Ki | = | 10.76 | nM | 7.97 |
| CHEMBL443979 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL66654 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL493568 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL468525 | — | Ki | = | 3330.0 | nM | 5.48 |
| CHEMBL501020 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL493776 | — | Ki | = | 7290.0 | nM | 5.14 |
| CHEMBL468526 | — | Ki | = | 7580.0 | nM | 5.12 |
| CHEMBL493775 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL464550 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL512634 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL493777 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL493571 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL292065 | — | Ki | - | — | - |