Assay Detail
Binding
CHEMBL4408248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by IonWork two-electrode voltage clamp method
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2A (CHEMBL1907604) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Neuroactive Steroid <i>N</i>-Methyl-d-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 6.73 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4555750 | — | — | 1 | 7.52 |
| CHEMBL4516765 | — | — | 1 | 7.48 |
| CHEMBL170154 | — | — | 1 | 7.43 |
| CHEMBL4513977 | — | — | 1 | 7.11 |
| CHEMBL4517382 | — | — | 1 | 7.10 |
| CHEMBL4450472 | — | — | 1 | 7.00 |
| CHEMBL4550075 | — | — | 1 | 6.92 |
| CHEMBL4586043 | — | — | 1 | 6.92 |
| CHEMBL171804 | — | — | 1 | 6.82 |
| CHEMBL2419157 | — | — | 1 | 6.75 |
| CHEMBL4475011 | — | — | 1 | 6.66 |
| CHEMBL4529930 | — | — | 1 | 6.57 |
| CHEMBL4567377 | — | — | 1 | 6.50 |
| CHEMBL4464591 | — | — | 1 | 6.50 |
| CHEMBL4468040 | — | — | 1 | 6.38 |
| CHEMBL4448829 | — | — | 1 | 6.32 |
| CHEMBL4439636 | — | — | 1 | 6.26 |
| CHEMBL4464781 | — | — | 1 | 6.05 |
| CHEMBL2419158 | — | — | 1 | 5.52 |
| CHEMBL4521106 | — | — | 1 | - |
| CHEMBL4476306 | — | — | 1 | - |
| CHEMBL4548602 | — | — | 1 | - |
| CHEMBL4522435 | — | — | 1 | - |
| CHEMBL4573975 | — | — | 1 | - |
| CHEMBL169046 | — | — | 1 | - |
| CHEMBL4579269 | — | — | 1 | - |
| CHEMBL4446143 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4555750 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4516765 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL170154 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4513977 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4517382 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4450472 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4550075 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4586043 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL171804 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2419157 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4475011 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4529930 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4567377 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4464591 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4468040 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4448829 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4439636 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4464781 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2419158 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4521106 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4476306 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4548602 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4522435 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4573975 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL169046 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4579269 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4446143 | — | EC50 | > | 10000.0 | nM | - |