Assay Detail
Binding
CHEMBL839720
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Binding affinity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells was determined by using [3H]MGS-0008
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Metabotropic glutamate receptor 2 (CHEMBL2851) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 61 | 8.24 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365305 | — | — | 1 | 8.97 |
| CHEMBL182972 | — | — | 1 | 8.84 |
| CHEMBL365680 | — | — | 1 | 8.83 |
| CHEMBL184983 | — | — | 1 | 8.79 |
| CHEMBL263312 | — | — | 1 | 8.75 |
| CHEMBL182899 | — | — | 1 | 8.70 |
| CHEMBL186630 | — | — | 1 | 8.64 |
| CHEMBL186453 | — | — | 1 | 8.62 |
| CHEMBL185210 | — | — | 1 | 8.60 |
| CHEMBL434536 | — | — | 1 | 8.59 |
| CHEMBL363724 | — | — | 1 | 8.58 |
| CHEMBL365647 | — | — | 1 | 8.53 |
| CHEMBL181710 | — | — | 1 | 8.52 |
| CHEMBL185423 | — | — | 1 | 8.51 |
| CHEMBL189814 | — | — | 1 | 8.50 |
| CHEMBL432038 | — | — | 1 | 8.50 |
| CHEMBL188787 | — | — | 1 | 8.48 |
| CHEMBL359491 | — | — | 1 | 8.45 |
| CHEMBL359905 | — | — | 1 | 8.44 |
| CHEMBL365244 | — | — | 1 | 8.43 |
| CHEMBL363696 | — | — | 1 | 8.42 |
| CHEMBL362459 | — | — | 1 | 8.42 |
| CHEMBL442967 | — | — | 1 | 8.41 |
| CHEMBL362325 | — | — | 1 | 8.40 |
| CHEMBL364320 | — | — | 1 | 8.39 |
| CHEMBL187482 | — | — | 1 | 8.37 |
| CHEMBL426983 | — | — | 1 | 8.37 |
| CHEMBL186107 | — | — | 1 | 8.36 |
| CHEMBL359805 | — | — | 1 | 8.34 |
| CHEMBL189186 | — | — | 1 | 8.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365305 | — | Ki | = | 1.06 | nM | 8.97 |
| CHEMBL182972 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL365680 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL184983 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL263312 | — | Ki | = | 1.79 | nM | 8.75 |
| CHEMBL182899 | — | Ki | = | 2.01 | nM | 8.70 |
| CHEMBL186630 | — | Ki | = | 2.27 | nM | 8.64 |
| CHEMBL186453 | — | Ki | = | 2.38 | nM | 8.62 |
| CHEMBL185210 | — | Ki | = | 2.53 | nM | 8.60 |
| CHEMBL434536 | — | Ki | = | 2.58 | nM | 8.59 |
| CHEMBL363724 | — | Ki | = | 2.61 | nM | 8.58 |
| CHEMBL365647 | — | Ki | = | 2.94 | nM | 8.53 |
| CHEMBL181710 | — | Ki | = | 3.05 | nM | 8.52 |
| CHEMBL185423 | — | Ki | = | 3.12 | nM | 8.51 |
| CHEMBL432038 | — | Ki | = | 3.13 | nM | 8.50 |
| CHEMBL189814 | — | Ki | = | 3.17 | nM | 8.50 |
| CHEMBL188787 | — | Ki | = | 3.28 | nM | 8.48 |
| CHEMBL359491 | — | Ki | = | 3.57 | nM | 8.45 |
| CHEMBL359905 | — | Ki | = | 3.67 | nM | 8.44 |
| CHEMBL365244 | — | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL363696 | — | Ki | = | 3.79 | nM | 8.42 |
| CHEMBL362459 | — | Ki | = | 3.77 | nM | 8.42 |
| CHEMBL442967 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL362325 | — | Ki | = | 4.02 | nM | 8.40 |
| CHEMBL364320 | — | Ki | = | 4.07 | nM | 8.39 |
| CHEMBL187482 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL426983 | — | Ki | = | 4.25 | nM | 8.37 |
| CHEMBL186107 | — | Ki | = | 4.35 | nM | 8.36 |
| CHEMBL359805 | — | Ki | = | 4.53 | nM | 8.34 |
| CHEMBL189186 | — | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL188511 | — | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL362092 | — | Ki | = | 4.99 | nM | 8.30 |
| CHEMBL434338 | — | Ki | = | 5.17 | nM | 8.29 |
| CHEMBL364201 | — | Ki | = | 5.36 | nM | 8.27 |
| CHEMBL189139 | — | Ki | = | 5.55 | nM | 8.26 |
| CHEMBL363980 | — | Ki | = | 5.61 | nM | 8.25 |
| CHEMBL183073 | — | Ki | = | 5.81 | nM | 8.24 |
| CHEMBL189710 | — | Ki | = | 5.72 | nM | 8.24 |
| CHEMBL362708 | — | Ki | = | 5.92 | nM | 8.23 |
| CHEMBL186145 | — | Ki | = | 6.68 | nM | 8.18 |
| CHEMBL188425 | — | Ki | = | 7.15 | nM | 8.15 |
| CHEMBL186214 | — | Ki | = | 7.14 | nM | 8.15 |
| CHEMBL361051 | — | Ki | = | 7.02 | nM | 8.15 |
| CHEMBL184441 | — | Ki | = | 7.07 | nM | 8.15 |
| CHEMBL366152 | — | Ki | = | 7.87 | nM | 8.10 |
| CHEMBL363940 | — | Ki | = | 8.57 | nM | 8.07 |
| CHEMBL185335 | — | Ki | = | 8.79 | nM | 8.06 |
| CHEMBL184504 | — | Ki | = | 9.34 | nM | 8.03 |
| CHEMBL186215 | — | Ki | = | 9.83 | nM | 8.01 |
| CHEMBL361024 | — | Ki | = | 11.8 | nM | 7.93 |