Assay Detail
Binding
CHEMBL4276582
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserine from serotonin 5-HT2A receptor in rat brain cortex homogenates incubated for 30 mins by liquid scintillation counting
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 7.27 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 9.74 |
| CHEMBL4290311 | — | — | 1 | 9.40 |
| CHEMBL4293999 | — | — | 1 | 9.14 |
| CHEMBL4289498 | — | — | 1 | 8.00 |
| CHEMBL4288409 | — | — | 1 | 7.76 |
| CHEMBL4281617 | — | — | 1 | 7.75 |
| CHEMBL4293659 | — | — | 1 | 7.72 |
| CHEMBL4283548 | — | — | 1 | 7.71 |
| CHEMBL4288766 | — | — | 1 | 7.70 |
| CHEMBL4276702 | — | — | 1 | 7.66 |
| CHEMBL4284435 | — | — | 1 | 7.65 |
| CHEMBL4284621 | — | — | 1 | 7.62 |
| CHEMBL4279363 | — | — | 1 | 7.53 |
| CHEMBL4285781 | — | — | 1 | 7.49 |
| CHEMBL4278627 | — | — | 1 | 7.46 |
| CHEMBL4292889 | — | — | 1 | 7.42 |
| CHEMBL4285041 | — | — | 1 | 7.30 |
| CHEMBL4287008 | — | — | 1 | 7.28 |
| CHEMBL4283488 | — | — | 1 | 7.23 |
| CHEMBL4291389 | — | — | 1 | 7.23 |
| CHEMBL4290422 | — | — | 1 | 7.23 |
| CHEMBL4286906 | — | — | 1 | 7.22 |
| CHEMBL4277770 | — | — | 1 | 7.17 |
| CHEMBL4294799 | — | — | 1 | 7.16 |
| CHEMBL4289001 | — | — | 1 | 7.14 |
| CHEMBL4290255 | — | — | 1 | 7.13 |
| CHEMBL4293347 | — | — | 1 | 7.10 |
| CHEMBL4288419 | — | — | 1 | 7.08 |
| CHEMBL4280873 | — | — | 1 | 7.08 |
| CHEMBL4288971 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4290311 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4293999 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL4289498 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL4288409 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL4281617 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL4293659 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL4283548 | — | Ki | = | 19.3 | nM | 7.71 |
| CHEMBL4288766 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL4276702 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL4284435 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL4284621 | — | Ki | = | 24.2 | nM | 7.62 |
| CHEMBL4279363 | — | Ki | = | 29.3 | nM | 7.53 |
| CHEMBL4285781 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL4278627 | — | Ki | = | 34.7 | nM | 7.46 |
| CHEMBL4292889 | — | Ki | = | 37.8 | nM | 7.42 |
| CHEMBL4285041 | — | Ki | = | 50.3 | nM | 7.30 |
| CHEMBL4287008 | — | Ki | = | 52.3 | nM | 7.28 |
| CHEMBL4283488 | — | Ki | = | 59.3 | nM | 7.23 |
| CHEMBL4291389 | — | Ki | = | 58.3 | nM | 7.23 |
| CHEMBL4290422 | — | Ki | = | 58.9 | nM | 7.23 |
| CHEMBL4286906 | — | Ki | = | 59.6 | nM | 7.22 |
| CHEMBL4277770 | — | Ki | = | 68.4 | nM | 7.17 |
| CHEMBL4294799 | — | Ki | = | 69.5 | nM | 7.16 |
| CHEMBL4289001 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL4290255 | — | Ki | = | 73.9 | nM | 7.13 |
| CHEMBL4293347 | — | Ki | = | 79.8 | nM | 7.10 |
| CHEMBL4288419 | — | Ki | = | 83.9 | nM | 7.08 |
| CHEMBL4280873 | — | Ki | = | 83.4 | nM | 7.08 |
| CHEMBL4288971 | — | Ki | = | 87.9 | nM | 7.06 |
| CHEMBL4281207 | — | Ki | = | 92.5 | nM | 7.03 |
| CHEMBL4286835 | — | Ki | = | 97.8 | nM | 7.01 |
| CHEMBL4276681 | — | Ki | = | 174.9 | nM | 6.76 |
| CHEMBL4289351 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL4294685 | — | Ki | = | 178.2 | nM | 6.75 |
| CHEMBL4278918 | — | Ki | = | 186.1 | nM | 6.73 |
| CHEMBL4286782 | — | Ki | = | 207.3 | nM | 6.68 |
| CHEMBL4287810 | — | Ki | = | 207.4 | nM | 6.68 |
| CHEMBL4291828 | — | Ki | = | 387.7 | nM | 6.41 |
| CHEMBL4295119 | — | Ki | = | 557.4 | nM | 6.25 |
| CHEMBL4284469 | — | Ki | = | 675.2 | nM | 6.17 |
| CHEMBL4293833 | — | Ki | = | 720.4 | nM | 6.14 |
| CHEMBL4279959 | — | Ki | = | 752.3 | nM | 6.12 |
| CHEMBL4282378 | — | Ki | = | 765.4 | nM | 6.12 |