Assay Detail
Binding
CHEMBL697805
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was tested for its affinity for Ionotropic glutamate receptor AMPA in in vitro binding assay on rat cortical membrane preparations using [3H]AMPA as ligand
31
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
8-Methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines: highly potent in vivo AMPA antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.23 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14861 | — | — | 3 | 8.40 |
| CHEMBL155485 | — | — | 1 | 7.75 |
| CHEMBL347566 | — | — | 1 | 7.72 |
| CHEMBL346259 | — | — | 1 | 7.43 |
| CHEMBL349553 | — | — | 1 | 7.07 |
| CHEMBL155029 | — | — | 1 | 6.96 |
| CHEMBL347246 | — | — | 1 | 6.89 |
| CHEMBL421990 | — | — | 1 | 6.75 |
| CHEMBL158137 | — | — | 1 | 6.60 |
| CHEMBL155386 | — | — | 1 | 6.52 |
| CHEMBL13260 | YM-90K | — | 1 | 6.46 |
| CHEMBL155075 | — | — | 1 | 6.35 |
| CHEMBL154355 | — | — | 1 | 6.21 |
| CHEMBL155558 | — | — | 1 | 6.17 |
| CHEMBL279116 | — | — | 1 | 6.12 |
| CHEMBL155438 | — | — | 1 | 6.05 |
| CHEMBL155609 | — | — | 1 | 6.01 |
| CHEMBL357967 | — | — | 1 | 5.90 |
| CHEMBL346735 | — | — | 1 | 5.70 |
| CHEMBL348307 | — | — | 1 | 5.52 |
| CHEMBL154387 | — | — | 1 | 5.49 |
| CHEMBL157713 | — | — | 1 | 5.48 |
| CHEMBL154469 | — | — | 1 | 5.25 |
| CHEMBL350693 | — | — | 1 | 4.80 |
| CHEMBL155437 | — | — | 1 | 4.77 |
| CHEMBL155025 | — | — | 1 | 4.52 |
| CHEMBL158194 | — | — | 1 | 4.52 |
| CHEMBL157242 | — | — | 1 | 4.00 |
| CHEMBL154330 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14861 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL14861 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL155485 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL347566 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL346259 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL14861 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL349553 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL155029 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL347246 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL421990 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL158137 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL155386 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL13260 | YM-90K | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL155075 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL154355 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL155558 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL279116 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL155438 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL155609 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL357967 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL346735 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL348307 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL154387 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL157713 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL154469 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL350693 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL155437 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL155025 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL158194 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL157242 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL154330 | — | IC50 | > | 100000.0 | nM | - |