Assay Detail
Functional
CHEMBL4008950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation of human mGluR5a expressed in CHO cells assessed as reduction in DHPG-induced cytosolic Ca2+ influx after 10 to 20 mins by fluo-4/AM-dye based fluorometric analysis
16
Total Activities
16
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
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.49 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4068928 | — | — | 1 | 7.92 |
| CHEMBL3763653 | — | — | 1 | 7.89 |
| CHEMBL4097994 | — | — | 1 | 7.70 |
| CHEMBL4081358 | — | — | 1 | 7.68 |
| CHEMBL4082155 | — | — | 1 | 7.66 |
| CHEMBL4070152 | — | — | 1 | 7.60 |
| CHEMBL4098854 | — | — | 1 | 7.60 |
| CHEMBL3764943 | — | — | 1 | 7.60 |
| CHEMBL4096394 | — | — | 1 | 7.57 |
| CHEMBL66654 | — | — | 1 | 7.51 |
| CHEMBL4091111 | — | — | 1 | 7.46 |
| CHEMBL4069140 | — | — | 1 | 7.37 |
| CHEMBL4080811 | — | — | 1 | 7.16 |
| CHEMBL4088680 | — | — | 1 | 7.13 |
| CHEMBL4090008 | — | — | 1 | 7.03 |
| CHEMBL3765114 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4068928 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3763653 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4097994 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4081358 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4082155 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4070152 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4098854 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3764943 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4096394 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL66654 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4091111 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4069140 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4080811 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4088680 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4090008 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3765114 | — | IC50 | = | 133.0 | nM | 6.88 |