Assay Detail
Binding
CHEMBL5328164
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human mGluR2 expressed in cell membrane incubated for 1 hr in presence of tritium labeled [3H]-7-((2,5-dioxopyrrolidin-1-yl)methyl)-4-(4-fluorophenyl)quinoline-2-carboxamide by competitive radioligand binding assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of [<sup>11</sup>C]MK-8056: A Selective PET Imaging Agent for the Study of mGluR<sub>2</sub> Negative Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.71 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3955188 | — | — | 1 | 9.72 |
| CHEMBL5405921 | — | — | 1 | 9.49 |
| CHEMBL3945590 | — | — | 1 | 9.34 |
| CHEMBL5409898 | — | — | 1 | 9.15 |
| CHEMBL5418895 | — | — | 1 | 9.13 |
| CHEMBL5429000 | — | — | 1 | 9.11 |
| CHEMBL5394450 | — | — | 1 | 9.10 |
| CHEMBL5435246 | — | — | 1 | 9.02 |
| CHEMBL5429261 | — | — | 1 | 9.00 |
| CHEMBL5436775 | — | — | 1 | 8.96 |
| CHEMBL3979547 | — | — | 1 | 8.96 |
| CHEMBL3950572 | — | — | 1 | 8.85 |
| CHEMBL5405655 | — | — | 1 | 8.82 |
| CHEMBL5410262 | — | — | 1 | 8.77 |
| CHEMBL3892073 | — | — | 1 | 8.74 |
| CHEMBL3895570 | — | — | 1 | 8.59 |
| CHEMBL5429002 | — | — | 1 | 8.35 |
| CHEMBL3910265 | — | — | 1 | 8.17 |
| CHEMBL5425858 | — | — | 1 | 8.15 |
| CHEMBL5399050 | — | — | 1 | 7.89 |
| CHEMBL3902752 | — | — | 1 | 7.82 |
| CHEMBL3981623 | — | — | 1 | 7.72 |
| CHEMBL3926904 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3955188 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL5405921 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL3945590 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL5409898 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL5418895 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL5429000 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL5394450 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL5435246 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL5429261 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5436775 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3979547 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3950572 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL5405655 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5410262 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3892073 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3895570 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL5429002 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL3910265 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL5425858 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5399050 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3902752 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3981623 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3926904 | — | Ki | = | 40.0 | nM | 7.40 |