Assay Detail
Functional
CHEMBL828431
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro potency against human recombinant mGlu5 receptor was determined by [Ca2+] flux assay using glutamate as agonist
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 |
|---|---|---|---|
| IC50 | 18 | 7.86 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184995 | — | — | 1 | 9.30 |
| CHEMBL369310 | — | — | 1 | 8.70 |
| CHEMBL185365 | — | — | 1 | 8.70 |
| CHEMBL182950 | — | — | 1 | 8.70 |
| CHEMBL183864 | — | — | 1 | 8.52 |
| CHEMBL63042 | — | — | 1 | 8.40 |
| CHEMBL362217 | — | — | 1 | 8.40 |
| CHEMBL292065 | — | — | 1 | 8.30 |
| CHEMBL181915 | — | — | 1 | 7.82 |
| CHEMBL182130 | — | — | 1 | 7.75 |
| CHEMBL185078 | — | — | 1 | 7.66 |
| CHEMBL183230 | — | — | 1 | 7.66 |
| CHEMBL181411 | — | — | 1 | 7.54 |
| CHEMBL365403 | — | — | 1 | 7.39 |
| CHEMBL65022 | — | — | 1 | 7.28 |
| CHEMBL303090 | — | — | 1 | 6.90 |
| CHEMBL183608 | — | — | 1 | 6.37 |
| CHEMBL185813 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184995 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL369310 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL185365 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL182950 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL183864 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL63042 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL362217 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL292065 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL181915 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL182130 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL185078 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL183230 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL181411 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL365403 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL65022 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL303090 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL183608 | — | IC50 | = | 423.0 | nM | 6.37 |
| CHEMBL185813 | — | IC50 | = | 845.0 | nM | 6.07 |