Assay Detail
Functional
CHEMBL4140822
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
15
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.22 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3609729 | — | — | 1 | 7.28 |
| CHEMBL4162576 | — | — | 1 | 6.97 |
| CHEMBL4160675 | — | — | 2 | 5.68 |
| CHEMBL1585091 | — | — | 1 | 5.50 |
| CHEMBL4164141 | — | — | 2 | - |
| CHEMBL4160748 | — | — | 2 | - |
| CHEMBL4168668 | — | — | 2 | - |
| CHEMBL4165248 | — | — | 2 | - |
| CHEMBL2361777 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3609729 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4162576 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL4160675 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4160675 | — | EC50 | = | 2137.96 | nM | 5.67 |
| CHEMBL1585091 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4164141 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL4160748 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4168668 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4165248 | — | EC50 | > | 30000.0 | nM | - |
| CHEMBL2361777 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2361777 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4165248 | — | EC50 | > | 31622.78 | nM | - |
| CHEMBL4168668 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4160748 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4164141 | — | EC50 | > | 31622.78 | nM | - |