Assay Detail
Binding
CHEMBL2213655
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Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
18
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.49 | 5.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204445 | — | — | 2 | 5.83 |
| CHEMBL2204442 | — | — | 2 | 5.69 |
| CHEMBL2204439 | — | — | 2 | 5.61 |
| CHEMBL2204446 | — | — | 2 | 5.49 |
| CHEMBL2204437 | — | — | 2 | 5.42 |
| CHEMBL2204436 | — | — | 1 | 5.38 |
| CHEMBL2204438 | — | — | 2 | 5.30 |
| CHEMBL2204440 | — | — | 2 | 5.24 |
| CHEMBL2204444 | — | — | 1 | - |
| CHEMBL2204443 | — | — | 1 | - |
| CHEMBL2204441 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204445 | — | IC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL2204445 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2204442 | — | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL2204442 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2204439 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL2204439 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2204446 | — | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL2204437 | — | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL2204437 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2204436 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2204438 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL2204438 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2204446 | — | IC50 | = | 5490.0 | nM | 5.26 |
| CHEMBL2204440 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2204440 | — | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL2204444 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2204443 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2204441 | — | IC50 | > | 10000.0 | nM | - |