Assay Detail
Binding
CHEMBL749677
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Displacement of racemic [3H]CP-101606 from rat forebrain membrane N-methyl-D-aspartate glutamate receptor 2B
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.36 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277787 | — | — | 1 | 7.77 |
| CHEMBL17703 | — | — | 2 | 7.75 |
| CHEMBL17198 | — | — | 1 | 7.70 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 7.57 |
| CHEMBL280083 | — | — | 2 | 7.51 |
| CHEMBL17833 | — | — | 1 | 7.46 |
| CHEMBL417630 | — | — | 1 | 6.97 |
| CHEMBL17909 | — | — | 1 | 6.89 |
| CHEMBL278666 | — | — | 1 | 6.52 |
| CHEMBL17933 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277787 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL17703 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL17198 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL17703 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL280083 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL17833 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL280083 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL417630 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL17909 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL278666 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL17933 | — | IC50 | > | 300.0 | nM | - |