Assay Detail
Binding
CHEMBL876376
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Displacement by compound of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.67 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183864 | — | — | 1 | 9.00 |
| CHEMBL369310 | — | — | 1 | 8.70 |
| CHEMBL184995 | — | — | 1 | 8.70 |
| CHEMBL63042 | — | — | 1 | 8.05 |
| CHEMBL182950 | — | — | 1 | 8.00 |
| CHEMBL292065 | — | — | 1 | 7.92 |
| CHEMBL182130 | — | — | 1 | 7.82 |
| CHEMBL365403 | — | — | 1 | 7.80 |
| CHEMBL362217 | — | — | 1 | 7.80 |
| CHEMBL181411 | — | — | 1 | 7.68 |
| CHEMBL183230 | — | — | 1 | 7.55 |
| CHEMBL185365 | — | — | 1 | 7.40 |
| CHEMBL185078 | — | — | 1 | 7.37 |
| CHEMBL181915 | — | — | 1 | 7.29 |
| CHEMBL65022 | — | — | 1 | 7.27 |
| CHEMBL183608 | — | — | 1 | 6.84 |
| CHEMBL303090 | — | — | 1 | 6.66 |
| CHEMBL185813 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183864 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL369310 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL184995 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL63042 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL182950 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL292065 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL182130 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL365403 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL362217 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL181411 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL183230 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL185365 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL185078 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL181915 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL65022 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL183608 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL303090 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL185813 | — | Ki | = | 638.0 | nM | 6.20 |