Assay Detail
Binding
CHEMBL4821480
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.16 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4866981 | — | — | 1 | 6.98 |
| CHEMBL4869198 | — | — | 1 | 6.90 |
| CHEMBL4867109 | — | — | 1 | 6.86 |
| CHEMBL4874914 | — | — | 1 | 6.79 |
| CHEMBL4470487 | — | — | 1 | 6.74 |
| CHEMBL4569757 | — | — | 1 | 6.52 |
| CHEMBL4439795 | — | — | 1 | 6.52 |
| CHEMBL4872713 | — | — | 1 | 6.50 |
| CHEMBL4860754 | — | — | 1 | 6.23 |
| CHEMBL4849583 | — | — | 1 | 6.16 |
| CHEMBL4565558 | — | — | 1 | 6.12 |
| CHEMBL4853700 | — | — | 1 | 5.84 |
| CHEMBL238916 | — | — | 1 | 5.65 |
| CHEMBL4860626 | — | — | 1 | 5.59 |
| CHEMBL4876545 | — | — | 1 | 5.32 |
| CHEMBL4873100 | — | — | 1 | 5.20 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 4.82 |
| CHEMBL4853248 | — | — | 1 | - |
| CHEMBL238917 | — | — | 1 | - |
| CHEMBL238915 | — | — | 1 | - |
| CHEMBL394110 | — | — | 1 | - |
| CHEMBL2107024 | REVOSPIRONE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4866981 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4869198 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL4867109 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL4874914 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL4470487 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL4569757 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL4439795 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL4872713 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL4860754 | — | Ki | = | 584.0 | nM | 6.23 |
| CHEMBL4849583 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL4565558 | — | Ki | = | 764.0 | nM | 6.12 |
| CHEMBL4853700 | — | Ki | = | 1438.0 | nM | 5.84 |
| CHEMBL238916 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL4860626 | — | Ki | = | 2580.0 | nM | 5.59 |
| CHEMBL4876545 | — | Ki | = | 4754.0 | nM | 5.32 |
| CHEMBL4873100 | — | Ki | = | 6306.0 | nM | 5.20 |
| CHEMBL8412 | IPSAPIRONE | Ki | = | 14980.0 | nM | 4.82 |
| CHEMBL4853248 | — | Ki | - | — | - | |
| CHEMBL238917 | — | Ki | - | — | - | |
| CHEMBL238915 | — | Ki | - | — | - | |
| CHEMBL394110 | — | Ki | - | — | - | |
| CHEMBL2107024 | REVOSPIRONE | Ki | - | — | - |