Assay Detail
Binding
CHEMBL899862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebellum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Metabotropic glutamate receptor 1 (CHEMBL4477) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of orally efficacious tetracyclic metabotropic glutamate receptor 1 (mGluR1) antagonists for the treatment of chronic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.14 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL241327 | — | — | 1 | 9.70 |
| CHEMBL236177 | — | — | 1 | 9.52 |
| CHEMBL236994 | — | — | 1 | 9.40 |
| CHEMBL393923 | — | — | 1 | 9.30 |
| CHEMBL235975 | — | — | 1 | 9.30 |
| CHEMBL235977 | — | — | 1 | 9.22 |
| CHEMBL393922 | — | — | 1 | 9.00 |
| CHEMBL236180 | — | — | 1 | 8.82 |
| CHEMBL238077 | — | — | 1 | 8.62 |
| CHEMBL428909 | — | — | 1 | 8.10 |
| CHEMBL236178 | — | — | 1 | 8.04 |
| CHEMBL394914 | — | — | 1 | 7.97 |
| CHEMBL393705 | — | — | 1 | 7.77 |
| CHEMBL238262 | — | — | 1 | 7.75 |
| CHEMBL238263 | — | — | 1 | 7.71 |
| CHEMBL238079 | — | — | 1 | 7.54 |
| CHEMBL238090 | — | — | 1 | 6.99 |
| CHEMBL235767 | — | — | 1 | 6.10 |
| CHEMBL429635 | — | — | 1 | 6.00 |
| CHEMBL392164 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL241327 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL236177 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL236994 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL393923 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL235975 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL235977 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL393922 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL236180 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL238077 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL428909 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL236178 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL394914 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL393705 | — | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL238262 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL238263 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL238079 | — | Ki | = | 28.6 | nM | 7.54 |
| CHEMBL238090 | — | Ki | = | 103.5 | nM | 6.99 |
| CHEMBL235767 | — | Ki | = | 788.0 | nM | 6.10 |
| CHEMBL429635 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL392164 | — | Ki | = | 1000.0 | nM | 6.00 |