Assay Detail
Binding
CHEMBL2162846
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human dopamine D2L 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 | 7.30 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.15 |
| CHEMBL2159491 | — | — | 1 | 8.10 |
| CHEMBL2159477 | — | — | 1 | 8.00 |
| CHEMBL2159492 | — | — | 1 | 8.00 |
| CHEMBL2159479 | — | — | 1 | 7.96 |
| CHEMBL2159467 | — | — | 1 | 7.82 |
| CHEMBL2159471 | — | — | 1 | 7.80 |
| CHEMBL2159489 | — | — | 1 | 7.80 |
| CHEMBL2159470 | — | — | 1 | 7.80 |
| CHEMBL2159483 | — | — | 1 | 7.75 |
| CHEMBL2159487 | — | — | 1 | 7.70 |
| CHEMBL2159469 | — | — | 1 | 7.62 |
| CHEMBL2159481 | — | — | 1 | 7.62 |
| CHEMBL2159485 | — | — | 1 | 7.60 |
| CHEMBL2159490 | — | — | 1 | 7.60 |
| CHEMBL2159455 | — | — | 1 | 7.50 |
| CHEMBL2159486 | — | — | 1 | 7.44 |
| CHEMBL2159488 | — | — | 1 | 7.41 |
| CHEMBL2159478 | — | — | 1 | 7.39 |
| CHEMBL2159458 | — | — | 1 | 7.34 |
| CHEMBL2159457 | — | — | 1 | 7.30 |
| CHEMBL2159461 | — | — | 1 | 7.30 |
| CHEMBL2159465 | — | — | 1 | 7.29 |
| CHEMBL2159484 | — | — | 1 | 7.22 |
| CHEMBL2159466 | — | — | 1 | 7.20 |
| CHEMBL2159460 | — | — | 1 | 7.18 |
| CHEMBL2159474 | — | — | 1 | 7.17 |
| CHEMBL2159472 | — | — | 1 | 7.14 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.14 |
| CHEMBL2159480 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2159491 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2159492 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159477 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159479 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2159467 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2159471 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2159489 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2159470 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2159483 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2159487 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2159469 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2159481 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2159485 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2159490 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2159455 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2159486 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL2159488 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL2159478 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL2159458 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2159457 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2159461 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2159465 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL2159484 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2159466 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2159460 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2159474 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL2159472 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL42 | CLOZAPINE | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL2159480 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL2159463 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL2159475 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL2159468 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL2159464 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL2159476 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL2159482 | — | Ki | = | 523.0 | nM | 6.28 |
| CHEMBL2159462 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL2159473 | — | Ki | = | 729.0 | nM | 6.14 |
| CHEMBL2159459 | — | Ki | = | 839.0 | nM | 6.08 |
| CHEMBL2159456 | — | Ki | = | 1059.0 | nM | 5.97 |