Assay Detail
Functional
CHEMBL1032406
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.62 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452618 | — | — | 1 | 8.59 |
| CHEMBL502882 | — | — | 1 | 8.24 |
| CHEMBL461673 | — | — | 1 | 8.20 |
| CHEMBL456823 | — | — | 1 | 8.15 |
| CHEMBL456196 | — | — | 1 | 8.14 |
| CHEMBL511355 | — | — | 1 | 8.01 |
| CHEMBL511352 | — | — | 1 | 7.96 |
| CHEMBL460827 | — | — | 1 | 7.80 |
| CHEMBL460391 | — | — | 1 | 7.75 |
| CHEMBL457026 | — | — | 1 | 7.41 |
| CHEMBL457872 | — | — | 1 | 7.31 |
| CHEMBL453249 | — | — | 1 | 7.26 |
| CHEMBL461034 | — | — | 1 | 7.24 |
| CHEMBL461035 | — | — | 1 | 6.92 |
| CHEMBL457873 | — | — | 1 | 6.66 |
| CHEMBL461033 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452618 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL502882 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL461673 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL456823 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL456196 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL511355 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL511352 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL460827 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL460391 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL457026 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL457872 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL453249 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL461034 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL461035 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL457873 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL461033 | — | IC50 | = | 590.0 | nM | 6.23 |