Assay Detail
Binding
CHEMBL1681232
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Displacement of [3H]MPEP from mGluR5 in rat brain
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.58 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229429 | — | — | 1 | 10.44 |
| CHEMBL446543 | — | — | 1 | 10.10 |
| CHEMBL1672272 | — | — | 1 | 9.60 |
| CHEMBL1672275 | — | — | 1 | 9.57 |
| CHEMBL1672288 | — | — | 1 | 9.55 |
| CHEMBL1672276 | — | — | 1 | 9.40 |
| CHEMBL1672271 | — | — | 1 | 9.05 |
| CHEMBL1672280 | — | — | 1 | 9.02 |
| CHEMBL1672284 | — | — | 1 | 8.89 |
| CHEMBL1672287 | — | — | 1 | 8.80 |
| CHEMBL1672277 | — | — | 1 | 8.51 |
| CHEMBL1672281 | — | — | 1 | 8.48 |
| CHEMBL1672279 | — | — | 1 | 8.43 |
| CHEMBL1672289 | — | — | 1 | 8.41 |
| CHEMBL1672283 | — | — | 1 | 8.38 |
| CHEMBL1672273 | — | — | 1 | 8.23 |
| CHEMBL1672278 | — | — | 1 | 8.09 |
| CHEMBL1672274 | — | — | 1 | 7.73 |
| CHEMBL1672282 | — | — | 1 | 7.65 |
| CHEMBL1671873 | — | — | 1 | 7.64 |
| CHEMBL1672285 | — | — | 1 | 7.63 |
| CHEMBL1672290 | — | — | 1 | 6.91 |
| CHEMBL1672286 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229429 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL446543 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL1672272 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL1672275 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL1672288 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1672276 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1672271 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1672280 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL1672284 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1672287 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1672277 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL1672281 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL1672279 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1672289 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1672283 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1672273 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL1672278 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL1672274 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL1672282 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL1671873 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL1672285 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL1672290 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1672286 | — | Ki | = | 132.9 | nM | 6.88 |