Assay Detail
Functional
CHEMBL1004110
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | HEK293-A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.94 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181483 | — | — | 1 | 9.38 |
| CHEMBL446543 | — | — | 1 | 9.09 |
| CHEMBL184995 | — | — | 1 | 8.92 |
| CHEMBL365403 | — | — | 1 | 8.52 |
| CHEMBL523693 | — | — | 1 | 8.51 |
| CHEMBL443979 | — | — | 1 | 8.46 |
| CHEMBL66654 | — | — | 1 | 8.45 |
| CHEMBL493569 | — | — | 1 | 8.34 |
| CHEMBL511603 | — | — | 1 | 8.32 |
| CHEMBL369310 | — | — | 1 | 8.28 |
| CHEMBL493773 | — | — | 1 | 8.21 |
| CHEMBL493774 | — | — | 1 | 8.14 |
| CHEMBL292065 | — | — | 1 | 7.87 |
| CHEMBL466006 | — | — | 1 | 7.86 |
| CHEMBL464372 | — | — | 1 | 7.66 |
| CHEMBL493568 | — | — | 1 | 7.60 |
| CHEMBL397121 | — | — | 1 | 7.01 |
| CHEMBL208927 | — | — | 1 | 6.31 |
| CHEMBL522507 | — | — | 1 | 6.19 |
| CHEMBL377829 | — | — | 1 | 5.73 |
| CHEMBL493777 | — | — | 1 | - |
| CHEMBL377935 | — | — | 1 | - |
| CHEMBL493572 | — | — | 1 | - |
| CHEMBL525384 | — | — | 1 | - |
| CHEMBL493573 | — | — | 1 | - |
| CHEMBL523856 | — | — | 1 | - |
| CHEMBL493570 | — | — | 1 | - |
| CHEMBL493571 | — | — | 1 | - |
| CHEMBL493775 | — | — | 1 | - |
| CHEMBL493776 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181483 | — | IC50 | = | 0.415 | nM | 9.38 |
| CHEMBL446543 | — | IC50 | = | 0.813 | nM | 9.09 |
| CHEMBL184995 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL365403 | — | IC50 | = | 3.05 | nM | 8.52 |
| CHEMBL523693 | — | IC50 | = | 3.08 | nM | 8.51 |
| CHEMBL443979 | — | IC50 | = | 3.43 | nM | 8.46 |
| CHEMBL66654 | — | IC50 | = | 3.54 | nM | 8.45 |
| CHEMBL493569 | — | IC50 | = | 4.57 | nM | 8.34 |
| CHEMBL511603 | — | IC50 | = | 4.83 | nM | 8.32 |
| CHEMBL369310 | — | IC50 | = | 5.24 | nM | 8.28 |
| CHEMBL493773 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL493774 | — | IC50 | = | 7.19 | nM | 8.14 |
| CHEMBL292065 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL466006 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL464372 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL493568 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL397121 | — | IC50 | = | 98.1 | nM | 7.01 |
| CHEMBL208927 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL522507 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL377829 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL468525 | — | IC50 | - | — | - | |
| CHEMBL468526 | — | IC50 | - | — | - | |
| CHEMBL464550 | — | IC50 | - | — | - | |
| CHEMBL501020 | — | IC50 | - | — | - | |
| CHEMBL467483 | — | IC50 | - | — | - | |
| CHEMBL467484 | — | IC50 | - | — | - | |
| CHEMBL467485 | — | IC50 | - | — | - | |
| CHEMBL469121 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL513699 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL512634 | — | IC50 | - | — | - | |
| CHEMBL493776 | — | IC50 | - | — | - | |
| CHEMBL493775 | — | IC50 | - | — | - | |
| CHEMBL493571 | — | IC50 | - | — | - | |
| CHEMBL493570 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL523856 | — | IC50 | - | — | - | |
| CHEMBL493573 | — | IC50 | - | — | - | |
| CHEMBL525384 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL493572 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL377935 | — | IC50 | - | — | - | |
| CHEMBL493777 | — | IC50 | - | — | - |