Assay Detail
Binding
CHEMBL617895
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor stably expressed in CHO cells
21
Total Activities
21
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
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.88 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL507898 | — | — | 1 | 8.30 |
| CHEMBL504699 | — | — | 1 | 8.00 |
| CHEMBL296512 | — | — | 1 | 7.80 |
| CHEMBL523245 | — | — | 1 | 7.72 |
| CHEMBL497877 | — | — | 1 | 7.72 |
| CHEMBL497064 | — | — | 1 | 7.32 |
| CHEMBL497054 | — | — | 1 | 7.30 |
| CHEMBL40584 | — | — | 1 | 7.10 |
| CHEMBL523760 | — | — | 1 | 7.07 |
| CHEMBL42557 | — | — | 1 | 7.05 |
| CHEMBL498729 | — | — | 1 | 6.88 |
| CHEMBL43819 | — | — | 1 | 6.82 |
| CHEMBL523585 | — | — | 1 | 6.81 |
| CHEMBL295559 | — | — | 1 | 6.40 |
| CHEMBL2113667 | — | — | 1 | 6.40 |
| CHEMBL497878 | — | — | 1 | 6.30 |
| CHEMBL46523 | — | — | 1 | 5.70 |
| CHEMBL43697 | — | — | 1 | 5.70 |
| CHEMBL44310 | — | — | 1 | 5.62 |
| CHEMBL295596 | — | — | 1 | 5.60 |
| CHEMBL507727 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL507898 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL504699 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL296512 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL523245 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL497877 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL497064 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL497054 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL40584 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL523760 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL42557 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL498729 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL43819 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL523585 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL295559 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL2113667 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL497878 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL46523 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL43697 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL44310 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL295596 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL507727 | — | Ki | > | 2000.0 | nM | - |