Assay Detail
Binding
CHEMBL4728769
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Negative allosteric modulation of human GluN1a/GluN2B receptor expressed in CHO cells assessed as inhibition of glutamate and glycine-induced calcium flux preincubated for 5 mins followed by glutamate and glycine addition and measured after 5 mins by calcium 5 dye based FLIPR assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| IC50 | 12 | 7.32 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4750166 | — | — | 1 | 8.22 |
| CHEMBL4460335 | — | — | 1 | 7.66 |
| CHEMBL4744919 | — | — | 1 | 7.60 |
| CHEMBL4762353 | — | — | 1 | 7.54 |
| CHEMBL4779889 | — | — | 1 | 7.51 |
| CHEMBL4800326 | — | — | 1 | 7.33 |
| CHEMBL4752661 | — | — | 1 | 7.15 |
| CHEMBL4776547 | — | — | 1 | 7.10 |
| CHEMBL4797865 | — | — | 1 | 7.09 |
| CHEMBL4797887 | — | — | 1 | 7.01 |
| CHEMBL4784055 | — | — | 1 | 6.93 |
| CHEMBL4799503 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4750166 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4460335 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4744919 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4762353 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4779889 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4800326 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4752661 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4776547 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4797865 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4797887 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4784055 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4799503 | — | IC50 | = | 216.0 | nM | 6.67 |