Assay Detail
Functional
CHEMBL832676
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity of compound against rat N-methyl-D-aspartate glutamate receptor using 11 nM [3H]glycine
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.10 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359908 | — | — | 1 | 8.05 |
| CHEMBL180427 | — | — | 1 | 7.96 |
| CHEMBL180317 | — | — | 1 | 7.85 |
| CHEMBL44793 | GAVESTINEL | 2.0 | 1 | 7.82 |
| CHEMBL179331 | — | — | 1 | 7.82 |
| CHEMBL180065 | — | — | 1 | 7.70 |
| CHEMBL426418 | — | — | 1 | 7.68 |
| CHEMBL180067 | — | — | 1 | 7.68 |
| CHEMBL361853 | — | — | 1 | 7.66 |
| CHEMBL180266 | — | — | 1 | 7.54 |
| CHEMBL362653 | — | — | 1 | 7.51 |
| CHEMBL359527 | — | — | 1 | 7.45 |
| CHEMBL179364 | — | — | 1 | 7.42 |
| CHEMBL180017 | — | — | 1 | 7.30 |
| CHEMBL179147 | — | — | 1 | 7.19 |
| CHEMBL178761 | — | — | 1 | 7.17 |
| CHEMBL362210 | — | — | 1 | 7.05 |
| CHEMBL361571 | — | — | 1 | 6.98 |
| CHEMBL425691 | — | — | 1 | 6.94 |
| CHEMBL178685 | — | — | 1 | 6.94 |
| CHEMBL179304 | — | — | 1 | 6.93 |
| CHEMBL179865 | — | — | 1 | 6.90 |
| CHEMBL179864 | — | — | 1 | 6.87 |
| CHEMBL359469 | — | — | 1 | 6.84 |
| CHEMBL176236 | — | — | 1 | 6.82 |
| CHEMBL179574 | — | — | 1 | 6.80 |
| CHEMBL359831 | — | — | 1 | 6.78 |
| CHEMBL179377 | — | — | 1 | 6.67 |
| CHEMBL178698 | — | — | 1 | 6.65 |
| CHEMBL179560 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359908 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL180427 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL180317 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL44793 | GAVESTINEL | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL179331 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL180065 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL426418 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL180067 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL361853 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL180266 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL362653 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL359527 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL179364 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL180017 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL179147 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL178761 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL362210 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL361571 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL425691 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL178685 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL179304 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL179865 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL179864 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL359469 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL176236 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL179574 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL359831 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL179377 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL178698 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL179560 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL175989 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL180467 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL178892 | — | IC50 | = | 1025.0 | nM | 5.99 |
| CHEMBL179261 | — | IC50 | = | 4664.0 | nM | 5.33 |