Assay Detail
Binding
CHEMBL1787493
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Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.08 | 9.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784599 | — | — | 1 | 9.97 |
| CHEMBL1784598 | — | — | 1 | 9.90 |
| CHEMBL1784618 | — | — | 1 | 9.70 |
| CHEMBL1784601 | — | — | 1 | 9.52 |
| CHEMBL1784540 | — | — | 1 | 9.44 |
| CHEMBL446543 | — | — | 1 | 9.44 |
| CHEMBL1784604 | — | — | 1 | 9.16 |
| CHEMBL1784541 | — | — | 1 | 9.03 |
| CHEMBL1784603 | — | — | 1 | 8.97 |
| CHEMBL1784602 | — | — | 1 | 8.73 |
| CHEMBL1784600 | — | — | 1 | 8.67 |
| CHEMBL292065 | — | — | 1 | 7.80 |
| CHEMBL66654 | — | — | 1 | 7.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784599 | — | Ki | = | 0.106 | nM | 9.97 |
| CHEMBL1784598 | — | Ki | = | 0.127 | nM | 9.90 |
| CHEMBL1784618 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1784601 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1784540 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL446543 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL1784604 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL1784541 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL1784603 | — | Ki | = | 1.06 | nM | 8.97 |
| CHEMBL1784602 | — | Ki | = | 1.84 | nM | 8.73 |
| CHEMBL1784600 | — | Ki | = | 2.14 | nM | 8.67 |
| CHEMBL292065 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL66654 | — | Ki | = | 18.7 | nM | 7.73 |