Assay Detail
Binding
CHEMBL2162845
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
40
Total Activities
40
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
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 6.49 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.40 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.30 |
| CHEMBL2159474 | — | — | 1 | 7.04 |
| CHEMBL2159480 | — | — | 1 | 7.02 |
| CHEMBL2159489 | — | — | 1 | 6.99 |
| CHEMBL2159472 | — | — | 1 | 6.99 |
| CHEMBL2159461 | — | — | 1 | 6.83 |
| CHEMBL2159484 | — | — | 1 | 6.81 |
| CHEMBL2159460 | — | — | 1 | 6.75 |
| CHEMBL2159486 | — | — | 1 | 6.73 |
| CHEMBL2159488 | — | — | 1 | 6.70 |
| CHEMBL2159487 | — | — | 1 | 6.70 |
| CHEMBL2159466 | — | — | 1 | 6.70 |
| CHEMBL2159475 | — | — | 1 | 6.65 |
| CHEMBL2159465 | — | — | 1 | 6.62 |
| CHEMBL2159485 | — | — | 1 | 6.61 |
| CHEMBL2159479 | — | — | 1 | 6.61 |
| CHEMBL2159470 | — | — | 1 | 6.59 |
| CHEMBL2159471 | — | — | 1 | 6.57 |
| CHEMBL2159492 | — | — | 1 | 6.57 |
| CHEMBL2159457 | — | — | 1 | 6.50 |
| CHEMBL2159458 | — | — | 1 | 6.50 |
| CHEMBL2159481 | — | — | 1 | 6.49 |
| CHEMBL2159478 | — | — | 1 | 6.45 |
| CHEMBL2159455 | — | — | 1 | 6.39 |
| CHEMBL2159477 | — | — | 1 | 6.30 |
| CHEMBL2159483 | — | — | 1 | 6.29 |
| CHEMBL2159490 | — | — | 1 | 6.27 |
| CHEMBL2159491 | — | — | 1 | 6.26 |
| CHEMBL2159462 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL715 | OLANZAPINE | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2159474 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL2159480 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL2159489 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL2159472 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL2159461 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL2159484 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL2159460 | — | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL2159486 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL2159487 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2159466 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL2159488 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL2159475 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL2159465 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL2159485 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL2159479 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL2159470 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL2159471 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL2159492 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL2159457 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL2159458 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL2159481 | — | Ki | = | 327.0 | nM | 6.49 |
| CHEMBL2159478 | — | Ki | = | 357.0 | nM | 6.45 |
| CHEMBL2159455 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL2159477 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL2159483 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL2159490 | — | Ki | = | 537.0 | nM | 6.27 |
| CHEMBL2159491 | — | Ki | = | 551.0 | nM | 6.26 |
| CHEMBL2159462 | — | Ki | = | 831.0 | nM | 6.08 |
| CHEMBL2159464 | — | Ki | = | 862.0 | nM | 6.06 |
| CHEMBL2159482 | — | Ki | = | 951.0 | nM | 6.02 |
| CHEMBL2159476 | — | Ki | = | 957.0 | nM | 6.02 |
| CHEMBL2159469 | — | Ki | = | 1335.0 | nM | 5.88 |
| CHEMBL2159467 | — | Ki | = | 1799.0 | nM | 5.75 |
| CHEMBL2159473 | — | Ki | = | 1779.0 | nM | 5.75 |
| CHEMBL2159468 | — | Ki | = | 1761.0 | nM | 5.75 |
| CHEMBL2159459 | — | Ki | = | 2124.0 | nM | 5.67 |
| CHEMBL2159456 | — | Ki | = | 2759.0 | nM | 5.56 |
| CHEMBL2159463 | — | Ki | = | 3785.0 | nM | 5.42 |