Assay Detail
Binding
CHEMBL3768173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]MPEP from rat mGlu5 receptor expressed in rat cerebrocortical membrane measured after 1 hr
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.91 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3764419 | — | — | 1 | 8.28 |
| CHEMBL3765114 | — | — | 1 | 8.28 |
| CHEMBL3763653 | — | — | 1 | 8.08 |
| CHEMBL3764138 | — | — | 1 | 8.02 |
| CHEMBL3764943 | — | — | 1 | 7.94 |
| CHEMBL3401575 | — | — | 1 | 7.82 |
| CHEMBL3765437 | — | — | 1 | 7.66 |
| CHEMBL3765747 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3764419 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL3765114 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3763653 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL3764138 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL3764943 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL3401575 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3765437 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3765747 | — | Ki | = | 68.0 | nM | 7.17 |