Assay Detail
Binding
CHEMBL5215990
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Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
12
Total Activities
12
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
Chemical update on the potential for serotonin 5-HT<sub>6</sub> and 5-HT<sub>7</sub> receptor agents in the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.09 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 9.60 |
| CHEMBL3329435 | PF-05212377 | 2.0 | 1 | 9.28 |
| CHEMBL362628 | — | — | 1 | 9.24 |
| CHEMBL1085113 | — | — | 1 | 9.20 |
| CHEMBL3286580 | IDALOPIRDINE | 3.0 | 1 | 9.08 |
| CHEMBL2103880 | CERLAPIRDINE | 2.0 | 1 | 8.89 |
| CHEMBL4117763 | — | — | 1 | 8.70 |
| CHEMBL392760 | — | — | 1 | 8.66 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 7.47 |
| CHEMBL1580288 | — | — | 1 | 6.92 |
| CHEMBL5219333 | — | — | 1 | 5.02 |
| CHEMBL5219968 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL3329435 | PF-05212377 | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL362628 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1085113 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL3286580 | IDALOPIRDINE | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL2103880 | CERLAPIRDINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4117763 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL392760 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL589390 | LATREPIRDINE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL1580288 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL5219333 | — | Ki | = | 9617.0 | nM | 5.02 |
| CHEMBL5219968 | — | Ki | = | 9967.0 | nM | 5.00 |