Assay Detail
Binding
CHEMBL4354014
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Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 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 |
| Cell Type | HEK293 |
| 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 | 7.52 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4435010 | — | — | 1 | 8.70 |
| CHEMBL4586990 | — | — | 1 | 8.52 |
| CHEMBL4574931 | — | — | 1 | 8.52 |
| CHEMBL4472629 | — | — | 1 | 8.40 |
| CHEMBL4471055 | — | — | 1 | 8.10 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 8.08 |
| CHEMBL4590882 | — | — | 1 | 8.05 |
| CHEMBL4552168 | — | — | 1 | 8.05 |
| CHEMBL4465638 | — | — | 1 | 8.05 |
| CHEMBL4451939 | — | — | 1 | 8.05 |
| CHEMBL4442332 | — | — | 1 | 8.00 |
| CHEMBL4461327 | — | — | 1 | 8.00 |
| CHEMBL4469792 | — | — | 1 | 8.00 |
| CHEMBL4513458 | — | — | 1 | 8.00 |
| CHEMBL4441060 | — | — | 1 | 8.00 |
| CHEMBL4566557 | — | — | 1 | 7.89 |
| CHEMBL4586353 | — | — | 1 | 7.85 |
| CHEMBL4521199 | — | — | 1 | 7.85 |
| CHEMBL4440402 | — | — | 1 | 7.85 |
| CHEMBL4469147 | — | — | 1 | 7.82 |
| CHEMBL4474829 | — | — | 1 | 7.82 |
| CHEMBL4466071 | — | — | 1 | 7.80 |
| CHEMBL4483304 | — | — | 1 | 7.77 |
| CHEMBL4592085 | — | — | 1 | 7.75 |
| CHEMBL4516784 | — | — | 1 | 7.72 |
| CHEMBL4520003 | — | — | 1 | 7.68 |
| CHEMBL4453733 | — | — | 1 | 7.68 |
| CHEMBL4453250 | — | — | 1 | 7.64 |
| CHEMBL4446215 | — | — | 1 | 7.60 |
| CHEMBL4469860 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4435010 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4586990 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4574931 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4472629 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4471055 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL715 | OLANZAPINE | Ki | = | 8.318 | nM | 8.08 |
| CHEMBL715 | OLANZAPINE | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL4590882 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4552168 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4451939 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4465638 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4513458 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4441060 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4469792 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4461327 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4442332 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4566557 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4586353 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4521199 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4440402 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4469147 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4474829 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4466071 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4483304 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4592085 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4516784 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4520003 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4453733 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4453250 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4446215 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4469860 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4571469 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4450907 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4459485 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL4451666 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4557068 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4470226 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL4546365 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL4455699 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4467359 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL4519004 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL4573880 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL4572629 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL4468396 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4468014 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4537701 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL4463737 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4442148 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4528162 | — | Ki | = | 263.0 | nM | 6.58 |
| CHEMBL4524906 | — | Ki | = | 280.0 | nM | 6.55 |