Assay Detail
Functional
CHEMBL869260
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against rat GluR1 flop expressed in Xenopus laevis oocyte assessed as inhibition of glutamate-induced current at holding potential -80 mV by two electrode voltage clamp method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Uncompetitive antagonism of AMPA receptors: Mechanistic insights from studies of polyamine toxin derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.87 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL213646 | — | — | 1 | 8.52 |
| CHEMBL213582 | — | — | 1 | 7.43 |
| CHEMBL213186 | — | — | 1 | 7.42 |
| CHEMBL212034 | — | — | 1 | 7.28 |
| CHEMBL213126 | — | — | 1 | 7.20 |
| CHEMBL385474 | — | — | 1 | 7.19 |
| CHEMBL214086 | — | — | 1 | 7.17 |
| CHEMBL213885 | — | — | 1 | 7.11 |
| CHEMBL211749 | — | — | 1 | 7.02 |
| CHEMBL214170 | — | — | 1 | 6.96 |
| CHEMBL378911 | — | — | 1 | 6.90 |
| CHEMBL213645 | — | — | 1 | 6.78 |
| CHEMBL214206 | — | — | 1 | 6.75 |
| CHEMBL213091 | — | — | 1 | 6.68 |
| CHEMBL214345 | — | — | 1 | 6.68 |
| CHEMBL212557 | — | — | 1 | 6.48 |
| CHEMBL215794 | — | — | 1 | 6.46 |
| CHEMBL214038 | — | — | 1 | 6.39 |
| CHEMBL379587 | — | — | 1 | 6.39 |
| CHEMBL384736 | — | — | 1 | 6.35 |
| CHEMBL425614 | — | — | 1 | 6.33 |
| CHEMBL213090 | — | — | 1 | 6.32 |
| CHEMBL377919 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL213646 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL213582 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL213186 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL212034 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL213126 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL385474 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL214086 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL213885 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL211749 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL214170 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL378911 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL213645 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL214206 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL213091 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL214345 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL212557 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL215794 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL214038 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL379587 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL384736 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL425614 | — | Ki | = | 468.0 | nM | 6.33 |
| CHEMBL213090 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL377919 | — | Ki | = | 685.0 | nM | 6.16 |