Assay Detail
Binding
CHEMBL4339649
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulation of recombinant human GluN1a/GluN2B expressed in CHO-T-REx cells assessed as inhibition of glutamate/glycine-induced response preincubated for 5 mins followed by glutamate/glycine addition and measured after 5 mins by calcium 5 dye based FLIPR TETRA analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.13 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4591770 | — | — | 1 | 7.82 |
| CHEMBL4443868 | — | — | 1 | 7.80 |
| CHEMBL4593473 | — | — | 1 | 7.77 |
| CHEMBL4547576 | — | — | 1 | 7.75 |
| CHEMBL4529074 | — | — | 1 | 7.68 |
| CHEMBL4460335 | — | — | 1 | 7.66 |
| CHEMBL4451514 | — | — | 1 | 7.64 |
| CHEMBL4302264 | — | — | 1 | 7.60 |
| CHEMBL4529810 | — | — | 1 | 7.54 |
| CHEMBL4445829 | — | — | 1 | 7.52 |
| CHEMBL4211247 | — | — | 1 | 7.50 |
| CHEMBL4474982 | — | — | 1 | 7.48 |
| CHEMBL4515350 | — | — | 1 | 7.43 |
| CHEMBL4475155 | — | — | 1 | 7.42 |
| CHEMBL4550955 | — | — | 1 | 7.39 |
| CHEMBL4451099 | — | — | 1 | 7.36 |
| CHEMBL4531750 | — | — | 1 | 7.33 |
| CHEMBL4590530 | — | — | 1 | 7.33 |
| CHEMBL4575739 | — | — | 1 | 7.27 |
| CHEMBL4446706 | — | — | 1 | 7.17 |
| CHEMBL4571666 | — | — | 1 | 7.09 |
| CHEMBL4526512 | — | — | 1 | 7.04 |
| CHEMBL4462073 | — | — | 1 | 6.84 |
| CHEMBL4588774 | — | — | 1 | 6.81 |
| CHEMBL4471014 | — | — | 1 | 6.75 |
| CHEMBL4464756 | — | — | 1 | 6.74 |
| CHEMBL4513602 | — | — | 1 | 6.44 |
| CHEMBL4467491 | — | — | 1 | 6.43 |
| CHEMBL4537967 | — | — | 1 | 6.40 |
| CHEMBL4539619 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4591770 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4443868 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4593473 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4547576 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4529074 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4460335 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4451514 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4302264 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4529810 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4445829 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4211247 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4474982 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4515350 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4475155 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4550955 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4451099 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4531750 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4590530 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4575739 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4446706 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4571666 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4526512 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4462073 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4588774 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4471014 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4464756 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4513602 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL4467491 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL4537967 | — | IC50 | = | 402.0 | nM | 6.40 |
| CHEMBL4539619 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL4462496 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL4442512 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4463483 | — | IC50 | = | 4460.0 | nM | 5.35 |