Assay Detail
Binding
CHEMBL3768172
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Displacement of [3H]MPEP from recombinant human mGluR5a expressed in A18 cells measured after 1 hr
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A18 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 2 | 7.53 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3764138 | — | — | 1 | 7.77 |
| CHEMBL3765747 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3764138 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3765747 | — | Ki | = | 52.0 | nM | 7.28 |