Assay Detail
Functional
CHEMBL711709
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Tested in vitro against human recombinant Metabotropic glutamate receptor 5 stably expressed in LtK cells by [Ca2+] flux assay using glutamate as antagonist
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | LtK |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.68 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66654 | — | — | 1 | 8.70 |
| CHEMBL292065 | — | — | 1 | 8.30 |
| CHEMBL63042 | — | — | 1 | 8.22 |
| CHEMBL65417 | — | — | 1 | 7.89 |
| CHEMBL65022 | — | — | 1 | 7.28 |
| CHEMBL65886 | — | — | 1 | 7.09 |
| CHEMBL63093 | — | — | 1 | 7.01 |
| CHEMBL303090 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66654 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL292065 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL63042 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL65417 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL65022 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL65886 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL63093 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL303090 | — | IC50 | = | 122.0 | nM | 6.91 |