Assay Detail
Binding
CHEMBL697364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand in rat cortical membrane preparations
27
Total Activities
25
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
Spiro-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives are mixed AMPA and NMDA glycine-site antagonists active in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.93 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14712 | — | — | 3 | 7.07 |
| CHEMBL329066 | — | — | 1 | 6.70 |
| CHEMBL13260 | YM-90K | — | 1 | 6.46 |
| CHEMBL329496 | — | — | 1 | 6.44 |
| CHEMBL98166 | — | — | 1 | 6.42 |
| CHEMBL330594 | — | — | 1 | 6.41 |
| CHEMBL318653 | — | — | 1 | 6.38 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 6.22 |
| CHEMBL421007 | — | — | 1 | 6.21 |
| CHEMBL99228 | — | — | 1 | 6.21 |
| CHEMBL279116 | — | — | 1 | 6.12 |
| CHEMBL330632 | — | — | 1 | 6.08 |
| CHEMBL319337 | — | — | 1 | 5.82 |
| CHEMBL98879 | — | — | 1 | 5.80 |
| CHEMBL319946 | — | — | 1 | 5.77 |
| CHEMBL98816 | — | — | 1 | 5.64 |
| CHEMBL316600 | — | — | 1 | 5.60 |
| CHEMBL100155 | — | — | 1 | 5.47 |
| CHEMBL328398 | — | — | 1 | 5.40 |
| CHEMBL99663 | — | — | 1 | 5.37 |
| CHEMBL98635 | — | — | 1 | 5.36 |
| CHEMBL98820 | — | — | 1 | 5.15 |
| CHEMBL317299 | — | — | 1 | 5.00 |
| CHEMBL99587 | — | — | 1 | 5.00 |
| CHEMBL318494 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14712 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL329066 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL14712 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL13260 | YM-90K | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL329496 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL98166 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL330594 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL318653 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL421007 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL99228 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL279116 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL330632 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL319337 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL98879 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL319946 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL98816 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL316600 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL100155 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL328398 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL99663 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL98635 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL14712 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL98820 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL317299 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL99587 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL318494 | — | IC50 | > | 10000.0 | nM | - |