Assay Detail
Functional
CHEMBL4479791
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Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 8.52 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4550190 | — | — | 1 | 9.70 |
| CHEMBL4560002 | — | — | 1 | 9.40 |
| CHEMBL4588437 | — | — | 1 | 9.22 |
| CHEMBL4580610 | — | — | 1 | 9.15 |
| CHEMBL3805542 | — | — | 1 | 9.10 |
| CHEMBL4517787 | — | — | 1 | 9.05 |
| CHEMBL4574977 | — | — | 1 | 8.92 |
| CHEMBL4556501 | — | — | 1 | 8.82 |
| CHEMBL4537236 | — | — | 1 | 8.82 |
| CHEMBL3804846 | — | — | 1 | 8.59 |
| CHEMBL4528135 | — | — | 1 | 8.48 |
| CHEMBL4554515 | — | — | 1 | 8.38 |
| CHEMBL4575547 | — | — | 1 | 8.32 |
| CHEMBL4545607 | — | — | 1 | 8.26 |
| CHEMBL3806078 | — | — | 1 | 8.22 |
| CHEMBL4552721 | — | — | 1 | 8.03 |
| CHEMBL4551992 | — | — | 1 | 8.00 |
| CHEMBL4578429 | — | — | 1 | 7.85 |
| CHEMBL4592158 | — | — | 1 | 7.60 |
| CHEMBL3805652 | — | — | 1 | 7.54 |
| CHEMBL4516570 | — | — | 1 | 7.42 |
| CHEMBL4571075 | BMS-984923 | 1.0 | 1 | - |
| CHEMBL4572894 | — | — | 1 | - |
| CHEMBL3805655 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4550190 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4560002 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4588437 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4580610 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3805542 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4517787 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4574977 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4556501 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4537236 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3804846 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4528135 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4554515 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4575547 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4545607 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3806078 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4552721 | — | EC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4551992 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4578429 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4592158 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3805652 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4516570 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4571075 | BMS-984923 | EC50 | > | 3000.0 | nM | - |
| CHEMBL4572894 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL3805655 | — | EC50 | > | 3000.0 | nM | - |