Assay Detail
Functional
CHEMBL4037493
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 39 | 5.42 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143210 | — | — | 1 | 7.64 |
| CHEMBL33567 | — | — | 1 | 6.54 |
| CHEMBL4067923 | — | — | 1 | 6.52 |
| CHEMBL4061423 | — | — | 1 | 6.29 |
| CHEMBL4088782 | — | — | 1 | 6.28 |
| CHEMBL4078629 | — | — | 1 | 6.01 |
| CHEMBL4091029 | — | — | 1 | 5.89 |
| CHEMBL4093492 | — | — | 1 | 5.82 |
| CHEMBL4075877 | — | — | 1 | 5.75 |
| CHEMBL4090179 | — | — | 1 | 5.72 |
| CHEMBL4072409 | — | — | 1 | 5.66 |
| CHEMBL4083240 | — | — | 1 | 5.60 |
| CHEMBL4075070 | — | — | 1 | 5.57 |
| CHEMBL4080400 | — | — | 1 | 5.54 |
| CHEMBL4101745 | — | — | 1 | 5.38 |
| CHEMBL4064187 | — | — | 1 | 5.36 |
| CHEMBL4069700 | — | — | 1 | 5.35 |
| CHEMBL4060017 | — | — | 1 | 5.34 |
| CHEMBL285043 | — | — | 1 | 5.29 |
| CHEMBL4077371 | — | — | 1 | 5.28 |
| CHEMBL4094241 | — | — | 1 | 5.27 |
| CHEMBL4101241 | — | — | 1 | 5.25 |
| CHEMBL4098424 | — | — | 1 | 5.18 |
| CHEMBL1089515 | — | — | 1 | 5.11 |
| CHEMBL4090312 | — | — | 1 | 5.08 |
| CHEMBL4076894 | — | — | 1 | 5.04 |
| CHEMBL4068205 | — | — | 1 | 4.85 |
| CHEMBL4061016 | — | — | 1 | 4.73 |
| CHEMBL4088251 | — | — | 1 | 4.70 |
| CHEMBL4100788 | — | — | 1 | 4.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143210 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL33567 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4067923 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4061423 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4088782 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4078629 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4091029 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4093492 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4075877 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4090179 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4072409 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4083240 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4075070 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4080400 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4101745 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4064187 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4069700 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4060017 | — | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL285043 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4077371 | — | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4094241 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4101241 | — | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4098424 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL1089515 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4090312 | — | EC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4076894 | — | EC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4068205 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4061016 | — | EC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL4088251 | — | EC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL4100788 | — | EC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL4074114 | — | EC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4076031 | — | EC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL4060360 | — | EC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL3114672 | — | EC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL4061539 | — | EC50 | = | 125000.0 | nM | - |
| CHEMBL4095462 | — | EC50 | = | 141000.0 | nM | - |
| CHEMBL4103332 | — | EC50 | = | 511000.0 | nM | - |
| CHEMBL4090699 | — | EC50 | = | 219000.0 | nM | - |
| CHEMBL4082270 | — | EC50 | > | 100000.0 | nM | - |