Assay Detail
Functional
CHEMBL4039214
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured after 1.9 mins by Fluo-4 AM dye based fluorescence assay
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Metabotropic glutamate receptor 5 (CHEMBL2564) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.65 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386849 | — | — | 2 | 8.51 |
| CHEMBL4077672 | — | — | 2 | 8.45 |
| CHEMBL4082854 | — | — | 2 | 8.17 |
| CHEMBL4096818 | — | — | 2 | 8.14 |
| CHEMBL4076771 | — | — | 2 | 8.04 |
| CHEMBL2386772 | — | — | 2 | 8.03 |
| CHEMBL4100830 | — | — | 2 | 8.02 |
| CHEMBL4093386 | — | — | 2 | 8.01 |
| CHEMBL2386850 | — | — | 2 | 7.97 |
| CHEMBL4095685 | — | — | 2 | 7.96 |
| CHEMBL4062697 | — | — | 2 | 7.72 |
| CHEMBL4103707 | — | — | 2 | 7.70 |
| CHEMBL2440659 | — | — | 2 | 7.62 |
| CHEMBL4084619 | — | — | 2 | 7.50 |
| CHEMBL2386771 | — | — | 2 | 7.48 |
| CHEMBL4070410 | — | — | 2 | 7.32 |
| CHEMBL4090661 | — | — | 2 | 7.27 |
| CHEMBL4071866 | — | — | 2 | 7.22 |
| CHEMBL4089038 | — | — | 2 | 7.01 |
| CHEMBL4076802 | — | — | 2 | 6.80 |
| CHEMBL3660237 | — | — | 2 | 6.70 |
| CHEMBL4076952 | — | — | 2 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386849 | — | IC50 | = | 3.09 | nM | 8.51 |
| CHEMBL2386849 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4077672 | — | IC50 | = | 3.548 | nM | 8.45 |
| CHEMBL4077672 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4082854 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4082854 | — | IC50 | = | 6.761 | nM | 8.17 |
| CHEMBL4096818 | — | IC50 | = | 7.244 | nM | 8.14 |
| CHEMBL4096818 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4076771 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4076771 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL2386772 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL2386772 | — | IC50 | = | 9.333 | nM | 8.03 |
| CHEMBL4100830 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4100830 | — | IC50 | = | 9.55 | nM | 8.02 |
| CHEMBL4093386 | — | IC50 | = | 9.772 | nM | 8.01 |
| CHEMBL4093386 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2386850 | — | IC50 | = | 10.72 | nM | 7.97 |
| CHEMBL4095685 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2386850 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4095685 | — | IC50 | = | 11.48 | nM | 7.94 |
| CHEMBL4062697 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4062697 | — | IC50 | = | 19.05 | nM | 7.72 |
| CHEMBL4103707 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4103707 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2440659 | — | IC50 | = | 23.99 | nM | 7.62 |
| CHEMBL2440659 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4084619 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4084619 | — | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL2386771 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2386771 | — | IC50 | = | 33.11 | nM | 7.48 |
| CHEMBL4070410 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4070410 | — | IC50 | = | 47.86 | nM | 7.32 |
| CHEMBL4090661 | — | IC50 | = | 53.7 | nM | 7.27 |
| CHEMBL4090661 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4071866 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4071866 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL4089038 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4089038 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL4076802 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4076802 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3660237 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3660237 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4076952 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4076952 | — | IC50 | = | 251.19 | nM | 6.60 |