Assay Detail
Binding
CHEMBL909969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AMPA from AMPA receptor in rat cortical synaptic membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.24 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL387049 | — | — | 1 | 7.37 |
| CHEMBL310286 | — | — | 1 | 6.60 |
| CHEMBL217826 | — | — | 1 | 6.30 |
| CHEMBL438473 | — | — | 1 | 5.89 |
| CHEMBL385648 | — | — | 1 | 5.38 |
| CHEMBL386418 | — | — | 1 | 5.21 |
| CHEMBL217551 | — | — | 1 | 5.08 |
| CHEMBL80594 | — | — | 1 | 4.94 |
| CHEMBL387402 | — | — | 1 | 4.78 |
| CHEMBL385438 | — | — | 1 | 4.78 |
| CHEMBL218290 | — | — | 1 | 4.44 |
| CHEMBL384572 | — | — | 1 | 4.35 |
| CHEMBL216390 | — | — | 1 | 4.22 |
| CHEMBL217073 | — | — | 1 | 4.00 |
| CHEMBL372797 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL387049 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL310286 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL217826 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL438473 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL385648 | — | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL386418 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL217551 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL80594 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL387402 | — | Ki | = | 16500.0 | nM | 4.78 |
| CHEMBL385438 | — | Ki | = | 16600.0 | nM | 4.78 |
| CHEMBL218290 | — | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL384572 | — | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL216390 | — | Ki | = | 60000.0 | nM | 4.22 |
| CHEMBL217073 | — | Ki | = | 99000.0 | nM | 4.00 |
| CHEMBL372797 | — | Ki | = | 117000.0 | nM | - |