Assay Detail
Binding
CHEMBL1839301
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
46
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT₆R) antagonists with unique structural features.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 7.63 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834337 | — | — | 1 | 8.57 |
| CHEMBL1834226 | — | — | 3 | 8.55 |
| CHEMBL1834342 | — | — | 1 | 8.39 |
| CHEMBL1834348 | — | — | 1 | 8.28 |
| CHEMBL1834338 | — | — | 1 | 8.25 |
| CHEMBL1834347 | — | — | 1 | 8.19 |
| CHEMBL1834350 | — | — | 1 | 8.14 |
| CHEMBL1834333 | — | — | 1 | 8.10 |
| CHEMBL1834341 | — | — | 1 | 8.10 |
| CHEMBL1834230 | — | — | 1 | 8.10 |
| CHEMBL1834238 | — | — | 1 | 8.09 |
| CHEMBL1834340 | — | — | 1 | 8.07 |
| CHEMBL1834235 | — | — | 1 | 8.03 |
| CHEMBL1834227 | — | — | 1 | 7.84 |
| CHEMBL1834241 | — | — | 1 | 7.77 |
| CHEMBL1834339 | — | — | 1 | 7.76 |
| CHEMBL1834228 | — | — | 1 | 7.75 |
| CHEMBL1834242 | — | — | 1 | 7.75 |
| CHEMBL1834240 | — | — | 1 | 7.73 |
| CHEMBL1834334 | — | — | 1 | 7.66 |
| CHEMBL1834229 | — | — | 1 | 7.62 |
| CHEMBL1834234 | — | — | 1 | 7.62 |
| CHEMBL1834345 | — | — | 1 | 7.62 |
| CHEMBL1834332 | — | — | 1 | 7.58 |
| CHEMBL1834243 | — | — | 1 | 7.56 |
| CHEMBL1834221 | — | — | 1 | 7.56 |
| CHEMBL1834225 | — | — | 1 | 7.47 |
| CHEMBL1834231 | — | — | 1 | 7.47 |
| CHEMBL1834346 | — | — | 1 | 7.30 |
| CHEMBL1834349 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834337 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1834226 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1834342 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL1834348 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL1834338 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL1834347 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL1834350 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL1834226 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL1834333 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL1834341 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL1834230 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1834238 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL1834340 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL1834235 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL1834227 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL1834226 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL1834241 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1834339 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL1834228 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL1834242 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL1834240 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL1834334 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL1834234 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL1834345 | — | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL1834229 | — | Ki | = | 24.2 | nM | 7.62 |
| CHEMBL1834332 | — | Ki | = | 26.6 | nM | 7.58 |
| CHEMBL1834243 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL1834221 | — | Ki | = | 27.8 | nM | 7.56 |
| CHEMBL1834225 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL1834231 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL1834346 | — | Ki | = | 49.9 | nM | 7.30 |
| CHEMBL1834349 | — | Ki | = | 71.1 | nM | 7.15 |
| CHEMBL1834222 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL1834351 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL1834335 | — | Ki | = | 119.4 | nM | 6.92 |
| CHEMBL1834239 | — | Ki | = | 138.1 | nM | 6.86 |
| CHEMBL1834352 | — | Ki | = | 146.6 | nM | 6.83 |
| CHEMBL1834336 | — | Ki | = | 196.7 | nM | 6.71 |
| CHEMBL1834232 | — | Ki | = | 231.1 | nM | 6.64 |
| CHEMBL1834237 | — | Ki | = | 321.8 | nM | 6.49 |
| CHEMBL1834343 | — | Ki | = | 510.1 | nM | 6.29 |
| CHEMBL1834344 | — | Ki | < | 6.0 | nM | - |
| CHEMBL1834223 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1834224 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1834233 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1834236 | — | Ki | > | 1000.0 | nM | - |