Assay Detail
Binding
CHEMBL3371192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 65 | 8.62 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3329438 | — | — | 1 | 10.40 |
| CHEMBL3329430 | — | — | 1 | 9.70 |
| CHEMBL3329451 | — | — | 1 | 9.70 |
| CHEMBL3329442 | — | — | 1 | 9.70 |
| CHEMBL3187365 | ASENAPINE | 4.0 | 1 | 9.60 |
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 9.60 |
| CHEMBL193400 | — | — | 1 | 9.52 |
| CHEMBL3329453 | — | — | 1 | 9.52 |
| CHEMBL3329452 | — | — | 1 | 9.52 |
| CHEMBL3329441 | — | — | 1 | 9.40 |
| CHEMBL372537 | — | — | 1 | 9.30 |
| CHEMBL3329429 | — | — | 1 | 9.30 |
| CHEMBL3329435 | PF-05212377 | 2.0 | 1 | 9.28 |
| CHEMBL1210710 | SB-399885 | — | 1 | 9.15 |
| CHEMBL29433 | — | — | 1 | 9.10 |
| CHEMBL3286580 | IDALOPIRDINE | 3.0 | 1 | 9.08 |
| CHEMBL3329450 | — | — | 1 | 9.05 |
| CHEMBL3329446 | — | — | 1 | 9.03 |
| CHEMBL3329449 | — | — | 1 | 9.00 |
| CHEMBL179814 | — | — | 1 | 9.00 |
| CHEMBL3329432 | — | — | 1 | 9.00 |
| CHEMBL3329440 | — | — | 1 | 9.00 |
| CHEMBL23038 | — | — | 1 | 9.00 |
| CHEMBL212995 | — | — | 1 | 8.92 |
| CHEMBL3329439 | — | — | 1 | 8.92 |
| CHEMBL3329434 | — | — | 1 | 8.92 |
| CHEMBL3329436 | — | — | 1 | 8.92 |
| CHEMBL431298 | — | — | 1 | 8.89 |
| CHEMBL2103880 | CERLAPIRDINE | 2.0 | 1 | 8.89 |
| CHEMBL361213 | — | — | 1 | 8.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3329438 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3329430 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3329442 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3329451 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3187365 | ASENAPINE | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL1083390 | INTEPIRDINE | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL193400 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3329453 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3329452 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3329441 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL372537 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3329429 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3329435 | PF-05212377 | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL1210710 | SB-399885 | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL29433 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3286580 | IDALOPIRDINE | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL3329450 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3329446 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL3329449 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL179814 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3329432 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3329440 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL23038 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3329436 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3329434 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL212995 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3329439 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL431298 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2103880 | CERLAPIRDINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL361213 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL92139 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3331585 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3329425 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3329447 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL76237 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL191429 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL361189 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL329383 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL93868 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL592752 | MARITUPIRDINE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3329443 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL1081794 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3329445 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL292759 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL177605 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL3329437 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL127411 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL3329448 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL367088 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL3329426 | — | Ki | = | 10.0 | nM | 8.00 |