Assay Detail
Binding
CHEMBL3594729
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GluN1/GluN2B receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of glutamate-evoked current by whole-cell voltage-clamp method
17
Total Activities
16
Compounds Tested
2
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/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
A New Class of Potent N-Methyl-D-Aspartate Receptor Inhibitors: Sulfated Neuroactive Steroids with Lipophilic D-Ring Modifications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.98 | 7.05 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593892 | — | — | 1 | 7.05 |
| CHEMBL3594108 | — | — | 1 | 6.77 |
| CHEMBL3594106 | — | — | 1 | 6.40 |
| CHEMBL3594107 | — | — | 1 | 6.30 |
| CHEMBL3594112 | — | — | 1 | 6.22 |
| CHEMBL3594109 | — | — | 1 | 6.22 |
| CHEMBL3594117 | — | — | 1 | 6.16 |
| CHEMBL3594113 | — | — | 1 | 6.10 |
| CHEMBL3594116 | — | — | 1 | 6.05 |
| CHEMBL3594115 | — | — | 1 | 5.96 |
| CHEMBL3594110 | — | — | 1 | 5.92 |
| CHEMBL3594111 | — | — | 1 | 5.80 |
| CHEMBL3594118 | — | — | 1 | 5.66 |
| CHEMBL3594120 | — | — | 1 | 5.27 |
| CHEMBL3594114 | — | — | 1 | 5.16 |
| CHEMBL1179566 | — | — | 2 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593892 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3594108 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3594106 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3594107 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3594112 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3594109 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3594117 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3594113 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3594116 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3594115 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3594110 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3594111 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3594118 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3594120 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3594114 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1179566 | — | IC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL1179566 | — | Inhibition | - | % | - |