Assay Detail
Binding
CHEMBL828708
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Inhibition of NMDA-evoked increased intracellular [Ca2+] in cells expressing NR1/NR2B receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Oxamides as novel NR2B selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.94 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL363722 | — | — | 1 | 8.70 |
| CHEMBL182665 | — | — | 1 | 8.52 |
| CHEMBL182066 | RADIPRODIL | 2.0 | 1 | 8.40 |
| CHEMBL317229 | — | — | 1 | 8.30 |
| CHEMBL363010 | — | — | 1 | 8.22 |
| CHEMBL183142 | — | — | 1 | 8.22 |
| CHEMBL367816 | — | — | 1 | 8.15 |
| CHEMBL219631 | BESONPRODIL | -1.0 | 1 | 8.10 |
| CHEMBL183825 | — | — | 1 | 8.10 |
| CHEMBL183457 | — | — | 1 | 8.05 |
| CHEMBL360463 | — | — | 1 | 8.00 |
| CHEMBL185812 | — | — | 1 | 7.82 |
| CHEMBL182951 | — | — | 1 | 7.75 |
| CHEMBL182369 | — | — | 1 | 7.54 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 7.52 |
| CHEMBL360373 | — | — | 1 | 7.51 |
| CHEMBL126228 | — | — | 1 | 7.38 |
| CHEMBL182698 | — | — | 1 | 7.32 |
| CHEMBL305195 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL363722 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL182665 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL182066 | RADIPRODIL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL317229 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL363010 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL183142 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL367816 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL219631 | BESONPRODIL | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL183825 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL183457 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL360463 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL185812 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL182951 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL182369 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL360373 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL126228 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL182698 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL305195 | — | IC50 | = | 57.0 | nM | 7.24 |