Assay Detail
Functional
CHEMBL893103
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Agonist activity at 5HT2A receptor in rat A7r5 cells assessed as intracellular calcium mobilization relative to 5HT
30
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | A7R5 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.20 | 8.44 |
| Emax | 12 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL394325 | — | — | 2 | 8.44 |
| CHEMBL232995 | — | — | 1 | 8.21 |
| CHEMBL234464 | — | — | 1 | 7.92 |
| CHEMBL101008 | — | — | 2 | 7.89 |
| CHEMBL234682 | — | — | 1 | 7.77 |
| CHEMBL134519 | — | — | 2 | 7.75 |
| CHEMBL394508 | — | — | 2 | 7.58 |
| CHEMBL391196 | — | — | 1 | 7.49 |
| CHEMBL393077 | — | — | 2 | 7.48 |
| CHEMBL234837 | — | — | 1 | 7.31 |
| CHEMBL397321 | — | — | 1 | 7.15 |
| CHEMBL234683 | — | — | 2 | 7.06 |
| CHEMBL394664 | — | — | 2 | 6.76 |
| CHEMBL232996 | — | — | 2 | 6.06 |
| CHEMBL232997 | — | — | 2 | 5.30 |
| CHEMBL397166 | — | — | 2 | 5.09 |
| CHEMBL234671 | — | — | 2 | - |
| CHEMBL232594 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL394325 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL232995 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL234464 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL101008 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL234682 | — | EC50 | = | 16.9 | nM | 7.77 |
| CHEMBL134519 | — | EC50 | = | 17.8 | nM | 7.75 |
| CHEMBL394508 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL391196 | — | EC50 | = | 32.7 | nM | 7.49 |
| CHEMBL393077 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL234837 | — | EC50 | = | 49.2 | nM | 7.31 |
| CHEMBL397321 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL234683 | — | EC50 | = | 87.8 | nM | 7.06 |
| CHEMBL394664 | — | EC50 | = | 175.0 | nM | 6.76 |
| CHEMBL232996 | — | EC50 | = | 880.0 | nM | 6.06 |
| CHEMBL232997 | — | EC50 | = | 4970.0 | nM | 5.30 |
| CHEMBL397166 | — | EC50 | = | 8192.0 | nM | 5.09 |
| CHEMBL394664 | — | Emax | = | 43.0 | % | - |
| CHEMBL101008 | — | Emax | = | 47.0 | % | - |
| CHEMBL232996 | — | Emax | = | 48.0 | % | - |
| CHEMBL234671 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL394508 | — | Emax | = | 40.0 | % | - |
| CHEMBL232997 | — | Emax | = | 45.0 | % | - |
| CHEMBL234671 | — | Emax | = | 15.0 | % | - |
| CHEMBL397166 | — | Emax | = | 27.0 | % | - |
| CHEMBL232594 | — | Emax | = | 7.0 | % | - |
| CHEMBL232594 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL393077 | — | Emax | = | 38.0 | % | - |
| CHEMBL394325 | — | Emax | = | 72.0 | % | - |
| CHEMBL234683 | — | Emax | = | 56.0 | % | - |
| CHEMBL134519 | — | Emax | = | 33.0 | % | - |