Assay Detail
Functional
CHEMBL1831599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | BHK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 50 | 6.35 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1830711 | — | — | 1 | 8.15 |
| CHEMBL1830707 | — | — | 1 | 8.05 |
| CHEMBL1830694 | — | — | 1 | 7.89 |
| CHEMBL1223381 | — | — | 1 | 7.70 |
| CHEMBL1830914 | — | — | 1 | 7.29 |
| CHEMBL1830695 | — | — | 1 | 7.25 |
| CHEMBL1830702 | — | — | 1 | 7.19 |
| CHEMBL1830915 | — | — | 1 | 7.00 |
| CHEMBL1830903 | — | — | 1 | 6.98 |
| CHEMBL1830900 | — | — | 1 | 6.85 |
| CHEMBL1830698 | — | — | 1 | 6.66 |
| CHEMBL562551 | — | — | 1 | 6.62 |
| CHEMBL1830906 | — | — | 1 | 6.54 |
| CHEMBL1830911 | — | — | 1 | 6.47 |
| CHEMBL1830910 | — | — | 1 | 6.41 |
| CHEMBL1830693 | — | — | 1 | 6.39 |
| CHEMBL1830912 | — | — | 1 | 6.22 |
| CHEMBL1830905 | — | — | 1 | 6.19 |
| CHEMBL1830902 | — | — | 1 | 6.12 |
| CHEMBL578988 | — | — | 1 | 6.12 |
| CHEMBL1830705 | — | — | 1 | 6.04 |
| CHEMBL1209431 | — | — | 1 | 6.00 |
| CHEMBL1830904 | — | — | 1 | 5.96 |
| CHEMBL1830709 | — | — | 1 | 5.89 |
| CHEMBL1830897 | — | — | 1 | 5.89 |
| CHEMBL515763 | — | — | 1 | 5.77 |
| CHEMBL1830701 | — | — | 1 | 5.66 |
| CHEMBL1830713 | — | — | 1 | 5.62 |
| CHEMBL1830909 | — | — | 1 | 5.57 |
| CHEMBL1830714 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1830711 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1830707 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1830694 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1223381 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1830914 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1830695 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1830702 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1830915 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1830903 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL1830900 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1830698 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL562551 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1830906 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1830911 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL1830910 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1830693 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1830912 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1830905 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1830902 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL578988 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1830705 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1209431 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1830904 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1830709 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1830897 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL515763 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1830701 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1830713 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1830909 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1830714 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL473806 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL507522 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1830712 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1830898 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1830697 | — | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1830907 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1830704 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830706 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830700 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830699 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830708 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830696 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830710 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830715 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830896 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830899 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830901 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830908 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830703 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1830913 | — | EC50 | > | 10000.0 | nM | - |