Assay Detail
Binding
CHEMBL752488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro affinity for N-methyl-D-aspartate glutamate receptor 1 using [3H]5,7-dichlorokynurenate([3H]-DCKA) 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 NMDA receptor (CHEMBL1907608) ↗| 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 | 4.89 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348307 | — | — | 1 | 6.75 |
| CHEMBL155609 | — | — | 1 | 6.00 |
| CHEMBL154330 | — | — | 1 | 5.68 |
| CHEMBL155386 | — | — | 1 | 5.64 |
| CHEMBL279116 | — | — | 1 | 5.52 |
| CHEMBL157713 | — | — | 1 | 5.28 |
| CHEMBL158137 | — | — | 1 | 5.11 |
| CHEMBL155558 | — | — | 1 | 5.08 |
| CHEMBL154387 | — | — | 1 | 5.00 |
| CHEMBL14861 | — | — | 3 | 5.00 |
| CHEMBL13260 | YM-90K | — | 1 | 5.00 |
| CHEMBL349553 | — | — | 1 | 5.00 |
| CHEMBL154469 | — | — | 1 | 4.66 |
| CHEMBL155485 | — | — | 1 | 4.00 |
| CHEMBL155029 | — | — | 1 | 4.00 |
| CHEMBL155438 | — | — | 1 | 4.00 |
| CHEMBL347566 | — | — | 1 | 4.00 |
| CHEMBL346259 | — | — | 1 | 4.00 |
| CHEMBL155437 | — | — | 1 | 4.00 |
| CHEMBL421990 | — | — | 1 | 4.00 |
| CHEMBL155075 | — | — | 1 | - |
| CHEMBL155025 | — | — | 1 | - |
| CHEMBL346735 | — | — | 1 | - |
| CHEMBL347246 | — | — | 1 | - |
| CHEMBL157242 | — | — | 1 | - |
| CHEMBL154355 | — | — | 1 | - |
| CHEMBL357967 | — | — | 1 | - |
| CHEMBL350693 | — | — | 1 | - |
| CHEMBL158194 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348307 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL155609 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL154330 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL155386 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL279116 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL157713 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL158137 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL155558 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL154387 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL349553 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL14861 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL14861 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL13260 | YM-90K | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL14861 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL154469 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL346259 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL155437 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL155485 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL155029 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL421990 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL347566 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL155438 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL155025 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL155075 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL346735 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL347246 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL157242 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL154355 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL357967 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL350693 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL158194 | — | IC50 | > | 100000.0 | nM | - |