Assay Detail
Binding
CHEMBL4354012
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHOK1 cells incubated for 1 hr by liquid scintillation counter method
54
Total Activities
53
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
2-Aminoimidazole-based antagonists of the 5-HT<sub>6</sub> receptor - A new concept in aminergic GPCR ligand design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 54 | 6.13 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 8.25 |
| CHEMBL4586353 | — | — | 1 | 7.00 |
| CHEMBL4469860 | — | — | 1 | 6.97 |
| CHEMBL4471055 | — | — | 1 | 6.31 |
| CHEMBL4516784 | — | — | 1 | 6.18 |
| CHEMBL4574931 | — | — | 1 | 6.17 |
| CHEMBL4435010 | — | — | 1 | 6.10 |
| CHEMBL4441060 | — | — | 1 | 6.05 |
| CHEMBL4451939 | — | — | 1 | 5.98 |
| CHEMBL4552168 | — | — | 1 | 5.95 |
| CHEMBL4472629 | — | — | 1 | 5.93 |
| CHEMBL4453733 | — | — | 1 | 5.91 |
| CHEMBL4442332 | — | — | 1 | 5.78 |
| CHEMBL4519004 | — | — | 1 | 5.72 |
| CHEMBL4450907 | — | — | 1 | 5.64 |
| CHEMBL4468014 | — | — | 1 | 5.61 |
| CHEMBL4463737 | — | — | 1 | 5.49 |
| CHEMBL4572629 | — | — | 1 | 5.29 |
| CHEMBL4483304 | — | — | 1 | 5.13 |
| CHEMBL4537701 | — | — | 1 | 5.10 |
| CHEMBL4519436 | — | — | 1 | - |
| CHEMBL4455699 | — | — | 1 | - |
| CHEMBL4557068 | — | — | 1 | - |
| CHEMBL4524906 | — | — | 1 | - |
| CHEMBL4548837 | — | — | 1 | - |
| CHEMBL4446215 | — | — | 1 | - |
| CHEMBL4442148 | — | — | 1 | - |
| CHEMBL4520003 | — | — | 1 | - |
| CHEMBL4470226 | — | — | 1 | - |
| CHEMBL4459485 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL715 | OLANZAPINE | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL4586353 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4469860 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL4471055 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL4516784 | — | Ki | = | 661.0 | nM | 6.18 |
| CHEMBL4574931 | — | Ki | = | 676.0 | nM | 6.17 |
| CHEMBL4435010 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL4441060 | — | Ki | = | 891.0 | nM | 6.05 |
| CHEMBL4451939 | — | Ki | = | 1047.0 | nM | 5.98 |
| CHEMBL4552168 | — | Ki | = | 1122.0 | nM | 5.95 |
| CHEMBL4472629 | — | Ki | = | 1175.0 | nM | 5.93 |
| CHEMBL4453733 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL4442332 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL4519004 | — | Ki | = | 1905.0 | nM | 5.72 |
| CHEMBL4450907 | — | Ki | = | 2291.0 | nM | 5.64 |
| CHEMBL4468014 | — | Ki | = | 2455.0 | nM | 5.61 |
| CHEMBL4463737 | — | Ki | = | 3236.0 | nM | 5.49 |
| CHEMBL4572629 | — | Ki | = | 5129.0 | nM | 5.29 |
| CHEMBL4483304 | — | Ki | = | 7413.0 | nM | 5.13 |
| CHEMBL4537701 | — | Ki | = | 7943.0 | nM | 5.10 |
| CHEMBL4528162 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4592085 | — | Ki | - | — | - | |
| CHEMBL4461327 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4571469 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4440402 | — | Ki | - | — | - | |
| CHEMBL4466071 | — | Ki | - | — | - | |
| CHEMBL4573880 | — | Ki | - | — | - | |
| CHEMBL4586990 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4519436 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4451666 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4521199 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4465638 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4566557 | — | Ki | - | — | - | |
| CHEMBL4474829 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4467359 | — | Ki | - | — | - | |
| CHEMBL4590882 | — | Ki | - | — | - | |
| CHEMBL4584746 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4446215 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4548837 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4524906 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4469147 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4557068 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4455699 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4442148 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4468396 | — | Ki | - | — | - | |
| CHEMBL4546365 | — | Ki | - | — | - | |
| CHEMBL4459485 | — | Ki | - | — | - | |
| CHEMBL4520003 | — | Ki | - | — | - | |
| CHEMBL4470226 | — | Ki | - | — | - |