Assay Detail
Binding
CHEMBL746726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at the glycine binding site of the N-methyl-D-aspartate glutamate receptor in rat cortical membranes using [3H]dichlorokynurenate ([3H]DCKA) as radioligand
40
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and sar of 2h-1,2,4-benzothiadiazine-1,1-dioxide-3- carboxylic acid derivatives as novel potent glycine antagonists of the nmda receptor-channel complex
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.38 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80741 | — | — | 3 | 8.40 |
| CHEMBL316115 | — | — | 1 | 8.10 |
| CHEMBL316074 | — | — | 1 | 8.05 |
| CHEMBL93771 | — | — | 1 | 7.96 |
| CHEMBL90410 | — | — | 1 | 7.92 |
| CHEMBL93104 | — | — | 1 | 7.92 |
| CHEMBL432051 | — | — | 1 | 7.89 |
| CHEMBL315882 | — | — | 1 | 7.85 |
| CHEMBL327243 | — | — | 1 | 7.77 |
| CHEMBL93636 | — | — | 1 | 7.75 |
| CHEMBL92881 | — | — | 1 | 7.70 |
| CHEMBL93318 | — | — | 1 | 7.70 |
| CHEMBL91355 | — | — | 1 | 7.70 |
| CHEMBL96805 | — | — | 1 | 7.68 |
| CHEMBL93394 | — | — | 1 | 7.66 |
| CHEMBL94240 | — | — | 1 | 7.58 |
| CHEMBL287327 | — | — | 1 | 7.58 |
| CHEMBL93738 | — | — | 1 | 7.54 |
| CHEMBL91694 | — | — | 1 | 7.48 |
| CHEMBL92782 | — | — | 1 | 7.44 |
| CHEMBL329167 | — | — | 1 | 7.42 |
| CHEMBL91680 | — | — | 1 | 7.40 |
| CHEMBL93470 | — | — | 1 | 7.39 |
| CHEMBL419319 | — | — | 1 | 7.36 |
| CHEMBL90980 | — | — | 1 | 7.35 |
| CHEMBL50267 | — | — | 1 | 7.34 |
| CHEMBL93379 | — | — | 1 | 7.32 |
| CHEMBL329656 | — | — | 1 | 7.32 |
| CHEMBL31344 | — | — | 1 | 7.30 |
| CHEMBL93528 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80741 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL316115 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL80741 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL316074 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL93771 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL90410 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL93104 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL432051 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL315882 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL327243 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL93636 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL93318 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL92881 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL91355 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL96805 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL93394 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL287327 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL94240 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL93738 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL91694 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL92782 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL329167 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL91680 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL93470 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL419319 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL90980 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL50267 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL93379 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL329656 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL31344 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL93528 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL94258 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL95039 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL94134 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL92527 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL329317 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL314550 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL80741 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL93527 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL92684 | — | IC50 | = | 9500.0 | nM | 5.02 |