Assay Detail
Binding
CHEMBL4058411
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse NR2B expressed in Hek293 cells co-expressing mouse NR1 assessed as inhibition of glutamic acid/glycine-induced intracellular Ca2+ levels measured after 1 day post induction by Fluo-3/AM dye-based fluorescence assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL3442) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of orally bioavailable cyclohexanol-based NR2B-selective NMDA receptor antagonists with analgesic activity utilizing a scaffold hopping approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.00 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4086848 | — | — | 1 | 9.20 |
| CHEMBL4094573 | — | — | 1 | 9.20 |
| CHEMBL4095807 | — | — | 1 | 9.00 |
| CHEMBL4078903 | — | — | 1 | 9.00 |
| CHEMBL4059534 | — | — | 1 | 8.70 |
| CHEMBL4069300 | — | — | 1 | 8.50 |
| CHEMBL4091437 | — | — | 1 | 8.50 |
| CHEMBL182066 | RADIPRODIL | 2.0 | 1 | 8.50 |
| CHEMBL4064453 | — | — | 1 | 8.20 |
| CHEMBL4076727 | — | — | 1 | 8.20 |
| CHEMBL4103672 | — | — | 1 | 8.00 |
| CHEMBL4065330 | — | — | 1 | 8.00 |
| CHEMBL4103723 | — | — | 1 | 7.90 |
| CHEMBL4065942 | — | — | 1 | 7.90 |
| CHEMBL4067110 | — | — | 1 | 7.80 |
| CHEMBL4102419 | — | — | 1 | 7.80 |
| CHEMBL4077427 | — | — | 1 | 7.80 |
| CHEMBL4076130 | — | — | 1 | 7.80 |
| CHEMBL4104737 | — | — | 1 | 7.80 |
| CHEMBL4093543 | — | — | 1 | 7.60 |
| CHEMBL4101281 | — | — | 1 | 7.60 |
| CHEMBL4073589 | — | — | 1 | 7.40 |
| CHEMBL4084983 | — | — | 1 | 7.40 |
| CHEMBL4074570 | — | — | 1 | 7.40 |
| CHEMBL4103182 | — | — | 1 | 7.20 |
| CHEMBL4063195 | — | — | 1 | 6.80 |
| CHEMBL4085797 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4086848 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL4094573 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL4095807 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4078903 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4059534 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4069300 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4091437 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL182066 | RADIPRODIL | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4064453 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4076727 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4103672 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4065330 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4103723 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4065942 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4067110 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4102419 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4077427 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4076130 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4104737 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4093543 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4101281 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4073589 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4084983 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4074570 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4103182 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4063195 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4085797 | — | IC50 | = | 199.53 | nM | 6.70 |