Assay Detail
Functional
CHEMBL904264
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at native AMPA receptor assessed as antagonism of (S)-5-fluoriwillardiine-induced depolarization of neonatal rat spinal cord motorneurones
3
Total Activities
3
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 |
|---|---|---|---|
| Kd | 3 | 4.12 | 4.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379442 | — | — | 1 | 4.15 |
| CHEMBL373428 | — | — | 1 | 4.08 |
| CHEMBL373429 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379442 | — | Kd | = | 71400.0 | nM | 4.15 |
| CHEMBL373428 | — | Kd | = | 83400.0 | nM | 4.08 |
| CHEMBL373429 | — | Kd | = | 108000.0 | nM | - |