Assay Detail
Binding
CHEMBL4354013
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Displacement of [3H]-methylspiperone from human D2 long 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 | 6.04 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL708 | ZIPRASIDONE | 4.0 | 2 | 9.07 |
| CHEMBL4441060 | — | — | 1 | 7.06 |
| CHEMBL4472629 | — | — | 1 | 6.15 |
| CHEMBL4586353 | — | — | 1 | 6.10 |
| CHEMBL4520003 | — | — | 1 | 5.93 |
| CHEMBL4471055 | — | — | 1 | 5.93 |
| CHEMBL4435010 | — | — | 1 | 5.92 |
| CHEMBL4572629 | — | — | 1 | 5.91 |
| CHEMBL4442332 | — | — | 1 | 5.88 |
| CHEMBL4469860 | — | — | 1 | 5.80 |
| CHEMBL4516784 | — | — | 1 | 5.79 |
| CHEMBL4519004 | — | — | 1 | 5.67 |
| CHEMBL4451939 | — | — | 1 | 5.63 |
| CHEMBL4455699 | — | — | 1 | 5.50 |
| CHEMBL4483304 | — | — | 1 | 5.44 |
| CHEMBL4463737 | — | — | 1 | 5.42 |
| CHEMBL4450907 | — | — | 1 | 5.40 |
| CHEMBL4453733 | — | — | 1 | 5.40 |
| CHEMBL4468396 | — | — | 1 | 5.29 |
| CHEMBL4469147 | — | — | 1 | 5.28 |
| CHEMBL4590882 | — | — | 1 | 5.15 |
| CHEMBL4558215 | — | — | 1 | - |
| CHEMBL4446215 | — | — | 1 | - |
| CHEMBL4519436 | — | — | 1 | - |
| CHEMBL4548837 | — | — | 1 | - |
| CHEMBL4524906 | — | — | 1 | - |
| CHEMBL4557068 | — | — | 1 | - |
| CHEMBL4442148 | — | — | 1 | - |
| CHEMBL4468014 | — | — | 1 | - |
| CHEMBL4470226 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL708 | ZIPRASIDONE | Ki | = | 0.8511 | nM | 9.07 |
| CHEMBL708 | ZIPRASIDONE | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL4441060 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL4472629 | — | Ki | = | 708.0 | nM | 6.15 |
| CHEMBL4586353 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL4471055 | — | Ki | = | 1175.0 | nM | 5.93 |
| CHEMBL4520003 | — | Ki | = | 1175.0 | nM | 5.93 |
| CHEMBL4435010 | — | Ki | = | 1202.0 | nM | 5.92 |
| CHEMBL4572629 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL4442332 | — | Ki | = | 1318.0 | nM | 5.88 |
| CHEMBL4469860 | — | Ki | = | 1585.0 | nM | 5.80 |
| CHEMBL4516784 | — | Ki | = | 1622.0 | nM | 5.79 |
| CHEMBL4519004 | — | Ki | = | 2138.0 | nM | 5.67 |
| CHEMBL4451939 | — | Ki | = | 2344.0 | nM | 5.63 |
| CHEMBL4455699 | — | Ki | = | 3162.0 | nM | 5.50 |
| CHEMBL4483304 | — | Ki | = | 3631.0 | nM | 5.44 |
| CHEMBL4463737 | — | Ki | = | 3802.0 | nM | 5.42 |
| CHEMBL4453733 | — | Ki | = | 3981.0 | nM | 5.40 |
| CHEMBL4450907 | — | Ki | = | 3981.0 | nM | 5.40 |
| CHEMBL4468396 | — | Ki | = | 5129.0 | nM | 5.29 |
| CHEMBL4469147 | — | Ki | = | 5248.0 | nM | 5.28 |
| CHEMBL4590882 | — | Ki | = | 7079.0 | nM | 5.15 |
| CHEMBL4528162 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4566557 | — | Ki | - | — | - | |
| CHEMBL4592085 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4461327 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4571469 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4440402 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4466071 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4573880 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4558215 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4584746 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4537701 | — | Ki | - | — | - | |
| CHEMBL4451666 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4521199 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4465638 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4467359 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4552168 | — | Ki | - | — | - | |
| CHEMBL4574931 | — | Ki | - | — | - | |
| CHEMBL4586990 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4546365 | — | Ki | - | — | - | |
| CHEMBL4459485 | — | Ki | - | — | - | |
| CHEMBL4470226 | — | Ki | - | — | - | |
| CHEMBL4468014 | — | Ki | - | — | - | |
| CHEMBL4442148 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4557068 | — | Ki | - | — | - | |
| CHEMBL4519436 | — | Ki | - | — | - | |
| CHEMBL4446215 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4548837 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4524906 | — | Ki | > | 10000.0 | nM | - |