Assay Detail
Binding
CHEMBL617075
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Binding affinity for displacement of [3H]ketanserin to human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 8.53 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83894 | FANANSERIN | 2.0 | 1 | 10.40 |
| CHEMBL504699 | — | — | 1 | 10.22 |
| CHEMBL74355 | VOLINANSERIN | 3.0 | 1 | 9.51 |
| CHEMBL145939 | — | — | 1 | 9.48 |
| CHEMBL357807 | — | — | 1 | 9.44 |
| CHEMBL146144 | — | — | 1 | 9.40 |
| CHEMBL146595 | — | — | 1 | 9.39 |
| CHEMBL358075 | — | — | 1 | 9.38 |
| CHEMBL146485 | — | — | 1 | 9.30 |
| CHEMBL148058 | — | — | 1 | 9.28 |
| CHEMBL146998 | — | — | 1 | 9.28 |
| CHEMBL147048 | — | — | 1 | 9.18 |
| CHEMBL148280 | — | — | 1 | 8.92 |
| CHEMBL149429 | — | — | 1 | 8.85 |
| CHEMBL146233 | — | — | 1 | 8.74 |
| CHEMBL147431 | — | — | 1 | 8.62 |
| CHEMBL146620 | — | — | 1 | 8.62 |
| CHEMBL150220 | — | — | 1 | 8.59 |
| CHEMBL150210 | — | — | 1 | 8.54 |
| CHEMBL148348 | — | — | 1 | 8.51 |
| CHEMBL149423 | — | — | 1 | 8.48 |
| CHEMBL147164 | — | — | 1 | 8.30 |
| CHEMBL343411 | — | — | 1 | 7.82 |
| CHEMBL148565 | — | — | 1 | 7.82 |
| CHEMBL359270 | — | — | 1 | 7.80 |
| CHEMBL148418 | — | — | 1 | 7.80 |
| CHEMBL122761 | — | — | 1 | 7.80 |
| CHEMBL149510 | — | — | 1 | 7.51 |
| CHEMBL423206 | — | — | 1 | 7.02 |
| CHEMBL148103 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83894 | FANANSERIN | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL504699 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL74355 | VOLINANSERIN | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL145939 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL357807 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL146144 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL146595 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL358075 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL146485 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL148058 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL146998 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL147048 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL148280 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL149429 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL146233 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL146620 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL147431 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL150220 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL150210 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL148348 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL149423 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL147164 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL343411 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL148565 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL359270 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL122761 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL148418 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL149510 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL423206 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL148103 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL358839 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL357883 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL146448 | — | Ki | > | 2000.0 | nM | - |