Assay Detail
Functional
CHEMBL904265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at native AMPA receptor assessed as fDR-VRP reduction of neonatal rat spinal cord motorneurones
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.75 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 6.67 |
| CHEMBL220822 | — | — | 1 | 5.55 |
| CHEMBL206407 | — | — | 1 | 4.93 |
| CHEMBL373428 | — | — | 1 | 4.79 |
| CHEMBL373429 | — | — | 1 | 4.78 |
| CHEMBL223841 | — | — | 1 | 4.73 |
| CHEMBL220509 | — | — | 1 | 4.60 |
| CHEMBL379442 | — | — | 1 | 4.51 |
| CHEMBL221321 | — | — | 1 | 4.37 |
| CHEMBL222521 | — | — | 1 | 4.29 |
| CHEMBL375004 | — | — | 1 | 4.26 |
| CHEMBL374553 | — | — | 1 | 4.19 |
| CHEMBL427186 | — | — | 1 | 4.13 |
| CHEMBL372797 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL220822 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL206407 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL373428 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL373429 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL223841 | — | IC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL220509 | — | IC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL379442 | — | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL221321 | — | IC50 | = | 42900.0 | nM | 4.37 |
| CHEMBL222521 | — | IC50 | = | 51200.0 | nM | 4.29 |
| CHEMBL375004 | — | IC50 | = | 55300.0 | nM | 4.26 |
| CHEMBL374553 | — | IC50 | = | 63900.0 | nM | 4.19 |
| CHEMBL427186 | — | IC50 | = | 74100.0 | nM | 4.13 |
| CHEMBL372797 | — | IC50 | = | 106000.0 | nM | - |