Assay Detail
Binding
CHEMBL2162843
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr
77
Total Activities
77
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 | 77 | 7.14 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2159465 | — | — | 1 | 9.52 |
| CHEMBL522691 | — | — | 1 | 9.24 |
| CHEMBL282199 | — | — | 1 | 8.92 |
| CHEMBL2159489 | — | — | 1 | 8.70 |
| CHEMBL95104 | — | — | 1 | 8.49 |
| CHEMBL2159488 | — | — | 1 | 8.40 |
| CHEMBL2159485 | — | — | 1 | 8.40 |
| CHEMBL2159322 | — | — | 1 | 8.30 |
| CHEMBL2159323 | — | — | 1 | 8.30 |
| CHEMBL2159487 | — | — | 1 | 8.22 |
| CHEMBL2159321 | — | — | 1 | 8.15 |
| CHEMBL2159481 | — | — | 1 | 8.15 |
| CHEMBL2159466 | — | — | 1 | 8.15 |
| CHEMBL2159483 | — | — | 1 | 8.05 |
| CHEMBL2159479 | — | — | 1 | 8.05 |
| CHEMBL2159471 | — | — | 1 | 8.00 |
| CHEMBL2159477 | — | — | 1 | 8.00 |
| CHEMBL2159492 | — | — | 1 | 8.00 |
| CHEMBL2159478 | — | — | 1 | 7.96 |
| CHEMBL2159491 | — | — | 1 | 7.92 |
| CHEMBL2159309 | — | — | 1 | 7.92 |
| CHEMBL2159458 | — | — | 1 | 7.89 |
| CHEMBL2159474 | — | — | 1 | 7.85 |
| CHEMBL2159486 | — | — | 1 | 7.82 |
| CHEMBL2159480 | — | — | 1 | 7.80 |
| CHEMBL2159484 | — | — | 1 | 7.80 |
| CHEMBL2159308 | — | — | 1 | 7.77 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.75 |
| CHEMBL2159455 | — | — | 1 | 7.70 |
| CHEMBL2159467 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2159465 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL522691 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL282199 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2159489 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL95104 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL2159488 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2159485 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2159323 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2159322 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2159487 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2159321 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2159481 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2159466 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2159483 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2159479 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2159471 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159492 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159477 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159478 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2159491 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2159309 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2159458 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2159474 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2159486 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2159484 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2159480 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2159308 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL42 | CLOZAPINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2159455 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2159467 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2159472 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2158033 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2159490 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2159470 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2159469 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL2159460 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2159475 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2159315 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2159457 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2159461 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL2159313 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL2159310 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL2159454 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL2159476 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL2159464 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL2159320 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL2159468 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL715 | OLANZAPINE | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL2159311 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL2159307 | — | Ki | = | 276.0 | nM | 6.56 |