Assay Detail
Binding
CHEMBL940926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]racemic CP-101606 from rat NR2B receptor in P2 membrane
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL311) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.86 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL246819 | — | — | 3 | 8.35 |
| CHEMBL401406 | — | — | 1 | 8.25 |
| CHEMBL247841 | — | — | 1 | 8.20 |
| CHEMBL247842 | — | — | 1 | 8.18 |
| CHEMBL246818 | — | — | 1 | 8.08 |
| CHEMBL246635 | — | — | 1 | 8.06 |
| CHEMBL246815 | — | — | 1 | 8.04 |
| CHEMBL247840 | — | — | 1 | 8.04 |
| CHEMBL404852 | — | — | 1 | 8.00 |
| CHEMBL404851 | — | — | 1 | 7.96 |
| CHEMBL246816 | — | — | 1 | 7.85 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 7.85 |
| CHEMBL246817 | — | — | 1 | 7.82 |
| CHEMBL247838 | — | — | 1 | 7.80 |
| CHEMBL401407 | — | — | 1 | 7.75 |
| CHEMBL247837 | — | — | 1 | 7.58 |
| CHEMBL246634 | — | — | 1 | 7.39 |
| CHEMBL246633 | — | — | 1 | 6.24 |
| CHEMBL247839 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL246819 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL401406 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL247841 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL247842 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL246819 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL246818 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL246635 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL246815 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL247840 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL404852 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL404851 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL246816 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL246817 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL247838 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL401407 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL246819 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL247837 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL246634 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL246633 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL247839 | — | IC50 | > | 5000.0 | nM | - |