Assay Detail
Functional
CHEMBL3412490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation of mGlu5 (unknown origin) expressed in HEK293 cells assessed as inhibition of L-AP4-induced calcium mobilization incubated for 30 mins prior to L-AP4 induction by Fluo-4 AM staining-based fluorescence assay
22
Total Activities
22
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
Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.11 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301626 | BASIMGLURANT | 2.0 | 1 | 8.15 |
| CHEMBL3410213 | — | — | 1 | 8.05 |
| CHEMBL3410223 | — | — | 1 | 8.00 |
| CHEMBL3410214 | — | — | 1 | 7.96 |
| CHEMBL3410220 | — | — | 1 | 7.92 |
| CHEMBL3410215 | — | — | 1 | 7.89 |
| CHEMBL3410224 | — | — | 1 | 7.80 |
| CHEMBL3410209 | — | — | 1 | 7.58 |
| CHEMBL3410216 | — | — | 1 | 7.55 |
| CHEMBL1946770 | — | — | 1 | 7.55 |
| CHEMBL3410217 | — | — | 1 | 7.16 |
| CHEMBL3410221 | — | — | 1 | 7.01 |
| CHEMBL3410218 | — | — | 1 | 7.00 |
| CHEMBL3410211 | — | — | 1 | 6.91 |
| CHEMBL3410219 | — | — | 1 | 6.85 |
| CHEMBL3410207 | — | — | 1 | 6.79 |
| CHEMBL3407528 | — | — | 1 | 6.53 |
| CHEMBL3410212 | — | — | 1 | 6.41 |
| CHEMBL3410225 | — | — | 1 | 6.31 |
| CHEMBL3410222 | — | — | 1 | 6.06 |
| CHEMBL3410208 | — | — | 1 | 5.60 |
| CHEMBL3410210 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301626 | BASIMGLURANT | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3410213 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3410223 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3410214 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3410220 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3410215 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3410224 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3410209 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3410216 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1946770 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3410217 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3410221 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3410218 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3410211 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3410219 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL3410207 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL3407528 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL3410212 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL3410225 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL3410222 | — | IC50 | = | 872.0 | nM | 6.06 |
| CHEMBL3410208 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3410210 | — | IC50 | = | 5600.0 | nM | 5.25 |