Assay Detail
Binding
CHEMBL2162844
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr
43
Total Activities
43
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 | 43 | 7.08 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2159486 | — | — | 1 | 8.30 |
| CHEMBL2159479 | — | — | 1 | 8.05 |
| CHEMBL2159484 | — | — | 1 | 8.00 |
| CHEMBL2159478 | — | — | 1 | 8.00 |
| CHEMBL2159472 | — | — | 1 | 7.89 |
| CHEMBL2159461 | — | — | 1 | 7.75 |
| CHEMBL2159470 | — | — | 1 | 7.68 |
| CHEMBL2159480 | — | — | 1 | 7.66 |
| CHEMBL2159489 | — | — | 1 | 7.66 |
| CHEMBL2159477 | — | — | 1 | 7.64 |
| CHEMBL2159474 | — | — | 1 | 7.55 |
| CHEMBL2159468 | — | — | 1 | 7.52 |
| CHEMBL2159485 | — | — | 1 | 7.51 |
| CHEMBL2159492 | — | — | 1 | 7.50 |
| CHEMBL2159471 | — | — | 1 | 7.35 |
| CHEMBL2159469 | — | — | 1 | 7.35 |
| CHEMBL2159467 | — | — | 1 | 7.32 |
| CHEMBL2159487 | — | — | 1 | 7.31 |
| CHEMBL2159476 | — | — | 1 | 7.19 |
| CHEMBL2159488 | — | — | 1 | 7.12 |
| CHEMBL2159483 | — | — | 1 | 7.09 |
| CHEMBL2159490 | — | — | 1 | 7.05 |
| CHEMBL2159481 | — | — | 1 | 7.04 |
| CHEMBL2159455 | — | — | 1 | 7.00 |
| CHEMBL2159460 | — | — | 1 | 6.98 |
| CHEMBL2159457 | — | — | 1 | 6.85 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.84 |
| CHEMBL2159491 | — | — | 1 | 6.83 |
| CHEMBL522691 | — | — | 1 | 6.73 |
| CHEMBL2159482 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2159486 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2159479 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2159478 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159484 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159472 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2159461 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2159470 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2159480 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2159489 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2159477 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2159474 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2159468 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2159485 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2159492 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2159469 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2159471 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2159467 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL2159487 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL2159476 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL2159488 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2159483 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL2159490 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL2159481 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL2159455 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL2159460 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL2159457 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL42 | CLOZAPINE | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL2159491 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL522691 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL2159482 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL2159464 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL95104 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2159473 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2159462 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL2159458 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL2159466 | — | Ki | = | 313.0 | nM | 6.50 |
| CHEMBL2159465 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL2159463 | — | Ki | = | 456.0 | nM | 6.34 |
| CHEMBL2159475 | — | Ki | = | 717.0 | nM | 6.14 |
| CHEMBL2159456 | — | Ki | = | 841.0 | nM | 6.08 |
| CHEMBL2159459 | — | Ki | = | 903.0 | nM | 6.04 |
| CHEMBL715 | OLANZAPINE | Ki | = | 3442.0 | nM | 5.46 |
| CHEMBL282199 | — | Ki | > | 5000.0 | nM | - |