Assay Detail
Functional
CHEMBL617043
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Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1D receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 8.57 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63167 | — | — | 1 | 9.70 |
| CHEMBL294732 | — | — | 1 | 9.40 |
| CHEMBL294547 | — | — | 1 | 9.22 |
| CHEMBL432332 | — | — | 1 | 9.05 |
| CHEMBL292779 | — | — | 1 | 9.00 |
| CHEMBL304857 | — | — | 1 | 8.82 |
| CHEMBL64004 | — | — | 1 | 8.80 |
| CHEMBL65321 | — | — | 1 | 8.72 |
| CHEMBL67684 | — | — | 1 | 8.59 |
| CHEMBL63432 | — | — | 1 | 8.42 |
| CHEMBL63799 | — | — | 1 | 8.30 |
| CHEMBL433108 | — | — | 1 | 7.80 |
| CHEMBL416688 | — | — | 1 | 7.75 |
| CHEMBL63258 | — | — | 1 | 7.47 |
| CHEMBL305301 | — | — | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63167 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL294732 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL294547 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL432332 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL292779 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL304857 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL64004 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL65321 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL67684 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL63432 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL63799 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL433108 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL416688 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL63258 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL305301 | — | EC50 | = | 35.0 | nM | 7.46 |