Assay Detail
Binding
CHEMBL1034751
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Metabotropic glutamate receptor 4 (CHEMBL2787) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.25 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL541754 | — | — | 1 | 7.10 |
| CHEMBL562551 | — | — | 1 | 6.96 |
| CHEMBL561835 | — | — | 1 | 6.68 |
| CHEMBL556667 | — | — | 1 | 6.54 |
| CHEMBL551635 | — | — | 1 | 6.43 |
| CHEMBL562036 | — | — | 1 | 6.30 |
| CHEMBL562232 | — | — | 1 | 6.13 |
| CHEMBL555454 | — | — | 1 | 6.00 |
| CHEMBL563423 | — | — | 1 | 5.77 |
| CHEMBL571453 | — | — | 1 | 5.75 |
| CHEMBL507522 | — | — | 1 | 5.69 |
| CHEMBL572346 | — | — | 1 | 5.62 |
| CHEMBL559271 | — | — | 1 | - |
| CHEMBL559960 | — | — | 1 | - |
| CHEMBL540427 | — | — | 1 | - |
| CHEMBL549669 | — | — | 1 | - |
| CHEMBL569148 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL541754 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL562551 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL561835 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL556667 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL551635 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL562036 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL562232 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL555454 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL563423 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL571453 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL507522 | — | EC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL572346 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL559271 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL559960 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL540427 | — | EC50 | - | — | - | |
| CHEMBL549669 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL569148 | — | EC50 | > | 10000.0 | nM | - |