Assay Detail
Functional
CHEMBL4136686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
24
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 7 (CHEMBL3879) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.01 | 6.29 |
| Activity | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4169114 | — | — | 3 | 6.29 |
| CHEMBL4174742 | — | — | 3 | 6.17 |
| CHEMBL4160395 | — | — | 3 | 6.15 |
| CHEMBL4176971 | — | — | 3 | 6.12 |
| CHEMBL4161847 | — | — | 3 | 6.11 |
| CHEMBL4165849 | — | — | 3 | 6.11 |
| CHEMBL4170997 | — | — | 3 | 5.87 |
| CHEMBL4160779 | — | — | 3 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4169114 | — | IC50 | = | 512.86 | nM | 6.29 |
| CHEMBL4169114 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4174742 | — | IC50 | = | 676.08 | nM | 6.17 |
| CHEMBL4174742 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL4160395 | — | IC50 | = | 707.95 | nM | 6.15 |
| CHEMBL4160395 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4176971 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4176971 | — | IC50 | = | 758.58 | nM | 6.12 |
| CHEMBL4161847 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4161847 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL4165849 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4165849 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL4170997 | — | IC50 | = | 1348.96 | nM | 5.87 |
| CHEMBL4170997 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4160779 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4160779 | — | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL4160395 | — | Activity | = | 11.0 | % | - |
| CHEMBL4165849 | — | Activity | = | 14.0 | % | - |
| CHEMBL4161847 | — | Activity | = | 19.0 | % | - |
| CHEMBL4170997 | — | Activity | = | 10.0 | % | - |
| CHEMBL4169114 | — | Activity | = | 11.0 | % | - |
| CHEMBL4176971 | — | Activity | = | 15.0 | % | - |
| CHEMBL4174742 | — | Activity | = | 8.0 | % | - |
| CHEMBL4160779 | — | Activity | = | 19.0 | % | - |