Assay Detail
Binding
CHEMBL5319830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation of human GluN1A/GluN2B receptor expressed in T-REX-CHO cells preincubated for 5 mins followed by glutamate and glycine addition and measured after 5 mins by FLIPR assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | T-REX-CHO |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of a Series of Substituted 1<i>H</i>-((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.17 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5410727 | — | — | 1 | 8.72 |
| CHEMBL5397778 | — | — | 1 | 8.46 |
| CHEMBL5433088 | — | — | 1 | 8.11 |
| CHEMBL5396805 | — | — | 1 | 8.08 |
| CHEMBL5438508 | — | — | 1 | 7.96 |
| CHEMBL5433511 | — | — | 1 | 7.96 |
| CHEMBL5421096 | — | — | 1 | 7.96 |
| CHEMBL5409770 | — | — | 1 | 7.80 |
| CHEMBL5413455 | — | — | 1 | 7.80 |
| CHEMBL5438363 | — | — | 1 | 7.80 |
| CHEMBL5414178 | — | — | 1 | 7.60 |
| CHEMBL5425798 | — | — | 1 | 7.31 |
| CHEMBL5432620 | — | — | 1 | 7.23 |
| CHEMBL5401297 | — | — | 1 | 6.89 |
| CHEMBL5399984 | — | — | 1 | 6.44 |
| CHEMBL5419741 | — | — | 1 | 6.41 |
| CHEMBL5426084 | — | — | 1 | 6.30 |
| CHEMBL5404498 | — | — | 1 | 6.24 |
| CHEMBL5432367 | — | — | 1 | 6.22 |
| CHEMBL5436548 | — | — | 1 | 6.11 |
| CHEMBL5395318 | — | — | 1 | 6.08 |
| CHEMBL5397475 | — | — | 1 | 5.92 |
| CHEMBL5433455 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5410727 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5397778 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5433088 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5396805 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5438508 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5433511 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5421096 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5409770 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5413455 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5438363 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5414178 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5425798 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5432620 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5401297 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5399984 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5419741 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5426084 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5404498 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5432367 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5436548 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL5395318 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL5397475 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5433455 | — | IC50 | = | 2500.0 | nM | 5.60 |