Assay Detail
Binding
CHEMBL2343303
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Displacement of [3H]-ABP688 from human mGluR5 expressed in HEK293 cells after 60 mins by scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.44 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66654 | — | — | 1 | 8.47 |
| CHEMBL2338580 | — | — | 1 | 7.52 |
| CHEMBL2338582 | — | — | 1 | 6.75 |
| CHEMBL2338590 | — | — | 1 | 6.69 |
| CHEMBL2338567 | — | — | 1 | 6.68 |
| CHEMBL2338566 | — | — | 1 | 6.50 |
| CHEMBL2338599 | — | — | 1 | 6.35 |
| CHEMBL2338569 | — | — | 1 | 6.31 |
| CHEMBL2338600 | — | — | 1 | 6.24 |
| CHEMBL2338571 | — | — | 1 | 6.17 |
| CHEMBL2338564 | — | — | 1 | 6.17 |
| CHEMBL2338565 | — | — | 1 | 6.12 |
| CHEMBL2338563 | — | — | 1 | 5.90 |
| CHEMBL2338587 | — | — | 1 | 5.89 |
| CHEMBL2338585 | — | — | 1 | 5.81 |
| CHEMBL2338575 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66654 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL2338580 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2338582 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL2338590 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL2338567 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL2338566 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2338599 | — | Ki | = | 445.0 | nM | 6.35 |
| CHEMBL2338569 | — | Ki | = | 492.0 | nM | 6.31 |
| CHEMBL2338600 | — | Ki | = | 582.0 | nM | 6.24 |
| CHEMBL2338571 | — | Ki | = | 674.0 | nM | 6.17 |
| CHEMBL2338564 | — | Ki | = | 672.0 | nM | 6.17 |
| CHEMBL2338565 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL2338563 | — | Ki | = | 1246.0 | nM | 5.90 |
| CHEMBL2338587 | — | Ki | = | 1275.0 | nM | 5.89 |
| CHEMBL2338585 | — | Ki | = | 1538.0 | nM | 5.81 |
| CHEMBL2338575 | — | Ki | = | 3790.0 | nM | 5.42 |