Assay Detail
Functional
CHEMBL3869550
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
35
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | AV12 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.10 | 7.84 |
| Imax | 17 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3913414 | — | — | 2 | 7.84 |
| CHEMBL3939492 | — | — | 2 | 7.69 |
| CHEMBL3969063 | — | — | 2 | 7.63 |
| CHEMBL3948272 | — | — | 2 | 7.53 |
| CHEMBL3977508 | — | — | 2 | 7.42 |
| CHEMBL3947221 | — | — | 2 | 7.34 |
| CHEMBL3933829 | — | — | 2 | 7.27 |
| CHEMBL3961306 | — | — | 2 | 7.15 |
| CHEMBL3956934 | — | — | 1 | 7.12 |
| CHEMBL3918170 | — | — | 2 | 7.08 |
| CHEMBL3927108 | — | — | 2 | 7.07 |
| CHEMBL3890112 | — | — | 2 | 6.90 |
| CHEMBL3971347 | — | — | 2 | 6.84 |
| CHEMBL3909237 | — | — | 2 | 6.82 |
| CHEMBL3953570 | — | — | 2 | 6.75 |
| CHEMBL3979475 | — | — | 2 | 6.73 |
| CHEMBL3955458 | — | — | 2 | 6.62 |
| CHEMBL3930511 | — | — | 2 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3913414 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL3939492 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL3969063 | — | IC50 | = | 23.5 | nM | 7.63 |
| CHEMBL3948272 | — | IC50 | = | 29.6 | nM | 7.53 |
| CHEMBL3977508 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL3947221 | — | IC50 | = | 46.1 | nM | 7.34 |
| CHEMBL3933829 | — | IC50 | = | 54.1 | nM | 7.27 |
| CHEMBL3961306 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3956934 | — | IC50 | = | 76.1 | nM | 7.12 |
| CHEMBL3918170 | — | IC50 | = | 83.2 | nM | 7.08 |
| CHEMBL3927108 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3890112 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3971347 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL3909237 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3953570 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL3979475 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL3955458 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL3930511 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL3977508 | — | Imax | > | 94.0 | % | - |
| CHEMBL3955458 | — | Imax | > | 94.0 | % | - |
| CHEMBL3953570 | — | Imax | > | 94.0 | % | - |
| CHEMBL3971347 | — | Imax | > | 94.0 | % | - |
| CHEMBL3909237 | — | Imax | > | 94.0 | % | - |
| CHEMBL3979475 | — | Imax | > | 94.0 | % | - |
| CHEMBL3918170 | — | Imax | > | 94.0 | % | - |
| CHEMBL3890112 | — | Imax | > | 94.0 | % | - |
| CHEMBL3927108 | — | Imax | > | 94.0 | % | - |
| CHEMBL3947221 | — | Imax | > | 94.0 | % | - |
| CHEMBL3961306 | — | Imax | > | 94.0 | % | - |
| CHEMBL3933829 | — | Imax | > | 94.0 | % | - |
| CHEMBL3930511 | — | Imax | > | 94.0 | % | - |
| CHEMBL3913414 | — | Imax | > | 94.0 | % | - |
| CHEMBL3939492 | — | Imax | > | 94.0 | % | - |
| CHEMBL3969063 | — | Imax | > | 94.0 | % | - |
| CHEMBL3948272 | — | Imax | > | 94.0 | % | - |