Assay Detail
Binding
CHEMBL4844529
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT<sub>3</sub> and 5-HT<sub>6</sub> Receptor Antagonist with Antipsychotic and Procognitive Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 8.12 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1210710 | SB-399885 | — | 1 | 9.15 |
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 8.85 |
| CHEMBL4865309 | — | — | 1 | 8.70 |
| CHEMBL4860809 | — | — | 1 | 8.70 |
| CHEMBL4872586 | — | — | 1 | 8.70 |
| CHEMBL4867565 | — | — | 1 | 8.52 |
| CHEMBL4125735 | — | — | 1 | 8.52 |
| CHEMBL4870374 | — | — | 1 | 8.52 |
| CHEMBL4862354 | — | — | 1 | 8.52 |
| CHEMBL4846153 | — | — | 1 | 8.52 |
| CHEMBL4853195 | — | — | 1 | 8.40 |
| CHEMBL4868468 | — | — | 1 | 8.30 |
| CHEMBL4161904 | — | — | 1 | 8.22 |
| CHEMBL4863272 | — | — | 1 | 8.15 |
| CHEMBL4872451 | — | — | 1 | 8.00 |
| CHEMBL4849693 | — | — | 1 | 7.96 |
| CHEMBL4861001 | — | — | 1 | 7.92 |
| CHEMBL4870340 | — | — | 1 | 7.89 |
| CHEMBL4847012 | — | — | 1 | 7.85 |
| CHEMBL4855043 | — | — | 1 | 7.85 |
| CHEMBL4847804 | — | — | 1 | 7.75 |
| CHEMBL4846691 | — | — | 1 | 7.75 |
| CHEMBL4864338 | — | — | 1 | 7.47 |
| CHEMBL4855303 | — | — | 1 | 6.61 |
| CHEMBL4877935 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1210710 | SB-399885 | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL1083390 | INTEPIRDINE | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4865309 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4860809 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4872586 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4867565 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4125735 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4870374 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4862354 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4846153 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4853195 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4868468 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4161904 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4863272 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4872451 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4849693 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4861001 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4870340 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4847012 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4855043 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4847804 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4846691 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4864338 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4855303 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL4877935 | — | Ki | = | 757.0 | nM | 6.12 |