Assay Detail
Binding
CHEMBL4728778
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3-[3H] 1-(azetidin-1-yl)-2-[6-(4-fluoro-3-methyl-phenyl)pyrrolo[3,2-b]pyridin-1-yl]ethanone from GluN1a/GluN2B receptor in rat cortex membranes measured after 2 hrs by liquid scintillation counting method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.50 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4762353 | — | — | 1 | 7.92 |
| CHEMBL4779889 | — | — | 1 | 7.80 |
| CHEMBL4797887 | — | — | 1 | 7.72 |
| CHEMBL4800326 | — | — | 1 | 7.72 |
| CHEMBL4750166 | — | — | 1 | 7.72 |
| CHEMBL4752661 | — | — | 1 | 7.68 |
| CHEMBL4784055 | — | — | 1 | 7.60 |
| CHEMBL4744919 | — | — | 1 | 7.36 |
| CHEMBL4776547 | — | — | 1 | 7.23 |
| CHEMBL4797865 | — | — | 1 | 7.20 |
| CHEMBL4799503 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4762353 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4779889 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4797887 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4800326 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4750166 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4752661 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4784055 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4744919 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL4776547 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4797865 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4799503 | — | Ki | = | 270.0 | nM | 6.57 |