Assay Detail
Functional
CHEMBL1046437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
25
Total Activities
25
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 | Intermediate |
Publication
Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.13 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569270 | — | — | 1 | 8.74 |
| CHEMBL577729 | — | — | 1 | 8.62 |
| CHEMBL566374 | — | — | 1 | 8.43 |
| CHEMBL566581 | — | — | 1 | 8.29 |
| CHEMBL572135 | — | — | 1 | 8.22 |
| CHEMBL568991 | — | — | 1 | 8.00 |
| CHEMBL567668 | — | — | 1 | 7.75 |
| CHEMBL578580 | — | — | 1 | 7.31 |
| CHEMBL568317 | — | — | 1 | 7.31 |
| CHEMBL577035 | — | — | 1 | 7.21 |
| CHEMBL584066 | — | — | 1 | 7.11 |
| CHEMBL576121 | — | — | 1 | 7.10 |
| CHEMBL567673 | — | — | 1 | 7.09 |
| CHEMBL579225 | — | — | 1 | 7.08 |
| CHEMBL579213 | — | — | 1 | 7.00 |
| CHEMBL567667 | — | — | 1 | 6.89 |
| CHEMBL565934 | — | — | 1 | 6.68 |
| CHEMBL571687 | — | — | 1 | 6.64 |
| CHEMBL572145 | — | — | 1 | 6.01 |
| CHEMBL579011 | — | — | 1 | 5.82 |
| CHEMBL568321 | — | — | 1 | 5.82 |
| CHEMBL572144 | — | — | 1 | 5.70 |
| CHEMBL577505 | — | — | 1 | 5.24 |
| CHEMBL572198 | — | — | 1 | - |
| CHEMBL576043 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569270 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL577729 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL566374 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL566581 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL572135 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL568991 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL567668 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL578580 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL568317 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL577035 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL584066 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL576121 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL567673 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL579225 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL579213 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL567667 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL565934 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL571687 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL572145 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL579011 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL568321 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL572144 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL577505 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL572198 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL576043 | — | IC50 | > | 10000.0 | nM | - |