Assay Detail
Binding
CHEMBL4821472
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Displacement of [3H]-5-OH-DPAT from human 5-HT1AR expressed in human HEK293 cells
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 42 | 7.80 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4875097 | — | — | 1 | 9.22 |
| CHEMBL4860626 | — | — | 1 | 9.00 |
| CHEMBL4849844 | — | — | 1 | 9.00 |
| CHEMBL2107024 | REVOSPIRONE | 2.0 | 1 | 8.70 |
| CHEMBL4876382 | — | — | 1 | 8.55 |
| CHEMBL4862246 | — | — | 1 | 8.52 |
| CHEMBL4860754 | — | — | 1 | 8.52 |
| CHEMBL4875803 | — | — | 1 | 8.49 |
| CHEMBL4856302 | — | — | 1 | 8.40 |
| CHEMBL4873100 | — | — | 1 | 8.22 |
| CHEMBL4860197 | — | — | 1 | 8.14 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 8.10 |
| CHEMBL292204 | — | — | 1 | 8.07 |
| CHEMBL4565558 | — | — | 1 | 8.00 |
| CHEMBL440466 | — | — | 1 | 8.00 |
| CHEMBL4853901 | — | — | 1 | 7.89 |
| CHEMBL4853700 | — | — | 1 | 7.89 |
| CHEMBL4866981 | — | — | 1 | 7.80 |
| CHEMBL4872713 | — | — | 1 | 7.80 |
| CHEMBL4867902 | — | — | 1 | 7.75 |
| CHEMBL4846523 | — | — | 1 | 7.70 |
| CHEMBL4849552 | — | — | 1 | 7.68 |
| CHEMBL4874914 | — | — | 1 | 7.68 |
| CHEMBL4871588 | — | — | 1 | 7.66 |
| CHEMBL4470487 | — | — | 1 | 7.62 |
| CHEMBL4869198 | — | — | 1 | 7.54 |
| CHEMBL4863131 | — | — | 1 | 7.42 |
| CHEMBL4877698 | — | — | 1 | 7.34 |
| CHEMBL4876545 | — | — | 1 | 7.11 |
| CHEMBL4867109 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4875097 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL4860626 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4849844 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2107024 | REVOSPIRONE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4876382 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL4862246 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4860754 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4875803 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL4856302 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4873100 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4860197 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL8412 | IPSAPIRONE | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL292204 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL4565558 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL440466 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4853901 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4853700 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4866981 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4872713 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4867902 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4846523 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4849552 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4874914 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4871588 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4470487 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4869198 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4863131 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4877698 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4876545 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4867109 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL238916 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2234893 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL2234891 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL27310 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4878835 | — | Ki | = | 402.0 | nM | 6.40 |
| CHEMBL4849583 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL26952 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4855300 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL238917 | — | Ki | - | — | - | |
| CHEMBL238915 | — | Ki | - | — | - | |
| CHEMBL394110 | — | Ki | - | — | - | |
| CHEMBL4853248 | — | Ki | > | 5000.0 | nM | - |