Assay Detail
Binding
CHEMBL4008945
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]M-MPEP from mGluR5 in Sprague-Dawley rat cerebrocortical membranes after 60 mins
29
Total Activities
29
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
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.69 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4081358 | — | — | 1 | 8.28 |
| CHEMBL4097994 | — | — | 1 | 8.19 |
| CHEMBL4098854 | — | — | 1 | 8.17 |
| CHEMBL3763653 | — | — | 1 | 8.08 |
| CHEMBL4096394 | — | — | 1 | 8.08 |
| CHEMBL66654 | — | — | 1 | 8.02 |
| CHEMBL3764138 | — | — | 1 | 8.02 |
| CHEMBL4091111 | — | — | 1 | 7.97 |
| CHEMBL3764943 | — | — | 1 | 7.94 |
| CHEMBL4068928 | — | — | 1 | 7.88 |
| CHEMBL4092590 | — | — | 1 | 7.80 |
| CHEMBL4082155 | — | — | 1 | 7.77 |
| CHEMBL4070152 | — | — | 1 | 7.75 |
| CHEMBL4069140 | — | — | 1 | 7.72 |
| CHEMBL4090008 | — | — | 1 | 7.52 |
| CHEMBL4080811 | — | — | 1 | 7.50 |
| CHEMBL4088680 | — | — | 1 | 7.49 |
| CHEMBL4100326 | — | — | 1 | 7.41 |
| CHEMBL3765114 | — | — | 1 | 7.26 |
| CHEMBL3765747 | — | — | 1 | 7.17 |
| CHEMBL4071804 | — | — | 1 | 7.15 |
| CHEMBL4063183 | — | — | 1 | 6.96 |
| CHEMBL4082312 | — | — | 1 | 6.75 |
| CHEMBL4105609 | — | — | 1 | - |
| CHEMBL4084830 | — | — | 1 | - |
| CHEMBL4074556 | — | — | 1 | - |
| CHEMBL4101273 | — | — | 1 | - |
| CHEMBL4102752 | — | — | 1 | - |
| CHEMBL4084032 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4081358 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL4097994 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4098854 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL3763653 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL4096394 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL66654 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL3764138 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL4091111 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL3764943 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL4068928 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL4092590 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4082155 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL4070152 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4069140 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL4090008 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL4080811 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL4088680 | — | Ki | = | 32.6 | nM | 7.49 |
| CHEMBL4100326 | — | Ki | = | 38.6 | nM | 7.41 |
| CHEMBL3765114 | — | Ki | = | 55.3 | nM | 7.26 |
| CHEMBL3765747 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4071804 | — | Ki | = | 71.2 | nM | 7.15 |
| CHEMBL4063183 | — | Ki | = | 110.4 | nM | 6.96 |
| CHEMBL4082312 | — | Ki | = | 179.6 | nM | 6.75 |
| CHEMBL4105609 | — | Ki | - | — | - | |
| CHEMBL4084830 | — | Ki | - | — | - | |
| CHEMBL4074556 | — | Ki | - | — | - | |
| CHEMBL4101273 | — | Ki | - | — | - | |
| CHEMBL4102752 | — | Ki | - | — | - | |
| CHEMBL4084032 | — | Ki | - | — | - |