Assay Detail
Binding
CHEMBL5142991
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Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Semisynthetic Transformations on (+)-Boldine Reveal a 5-HT<sub>2A/2C</sub>R Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.57 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5195241 | — | — | 1 | 7.70 |
| CHEMBL5204813 | — | — | 1 | 7.66 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.62 |
| CHEMBL5180016 | — | — | 1 | 7.00 |
| CHEMBL5183799 | — | — | 1 | 6.86 |
| CHEMBL5175973 | — | — | 1 | 6.81 |
| CHEMBL5174366 | — | — | 1 | 6.73 |
| CHEMBL5194057 | — | — | 1 | 6.67 |
| CHEMBL3581255 | — | — | 1 | 6.67 |
| CHEMBL5185086 | — | — | 1 | 6.62 |
| CHEMBL3580670 | — | — | 1 | 6.62 |
| CHEMBL3581250 | — | — | 1 | 6.61 |
| CHEMBL5203303 | — | — | 1 | 6.61 |
| CHEMBL3581245 | — | — | 1 | 6.57 |
| CHEMBL5188171 | — | — | 1 | 6.53 |
| CHEMBL3581249 | — | — | 1 | 6.42 |
| CHEMBL3581254 | — | — | 1 | 6.42 |
| CHEMBL3581256 | — | — | 1 | 6.38 |
| CHEMBL3581251 | — | — | 1 | 6.35 |
| CHEMBL5181312 | — | — | 1 | 6.29 |
| CHEMBL5208882 | — | — | 1 | 6.27 |
| CHEMBL3581246 | — | — | 1 | 6.24 |
| CHEMBL3581252 | — | — | 1 | 6.24 |
| CHEMBL3581253 | — | — | 1 | 6.24 |
| CHEMBL5184659 | — | — | 1 | 6.23 |
| CHEMBL3581248 | — | — | 1 | 6.12 |
| CHEMBL3581244 | — | — | 1 | 6.09 |
| CHEMBL228082 | GLAUCINE | — | 1 | 6.01 |
| CHEMBL3581247 | — | — | 1 | 5.94 |
| CHEMBL5187013 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5195241 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5204813 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL42 | CLOZAPINE | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL5180016 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL5183799 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL5175973 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL5174366 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL5194057 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL3581255 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL5185086 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL3580670 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL3581250 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL5203303 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL3581245 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL5188171 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL3581249 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL3581254 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL3581256 | — | Ki | = | 418.0 | nM | 6.38 |
| CHEMBL3581251 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL5181312 | — | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL5208882 | — | Ki | = | 534.0 | nM | 6.27 |
| CHEMBL3581246 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL3581252 | — | Ki | = | 582.0 | nM | 6.24 |
| CHEMBL3581253 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL5184659 | — | Ki | = | 587.0 | nM | 6.23 |
| CHEMBL3581248 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL3581244 | — | Ki | = | 818.0 | nM | 6.09 |
| CHEMBL228082 | GLAUCINE | Ki | = | 966.0 | nM | 6.01 |
| CHEMBL3581247 | — | Ki | = | 1156.0 | nM | 5.94 |
| CHEMBL5187013 | — | Ki | - | — | - |