Assay Detail
Binding
CHEMBL616929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in Chinese hamster ovary cells (CHO cells)
11
Total Activities
11
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 | Expert |
Publication
Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.24 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL313714 | — | — | 1 | 9.05 |
| CHEMBL343492 | — | — | 1 | 8.85 |
| CHEMBL138872 | — | — | 1 | 8.70 |
| CHEMBL139801 | — | — | 1 | 8.47 |
| CHEMBL343105 | — | — | 1 | 8.43 |
| CHEMBL441095 | — | — | 1 | 8.34 |
| CHEMBL138873 | — | — | 1 | 8.25 |
| CHEMBL138821 | — | — | 1 | 8.14 |
| CHEMBL343712 | — | — | 1 | 7.66 |
| CHEMBL138462 | — | — | 1 | 7.50 |
| CHEMBL139438 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL313714 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL343492 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL138872 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL139801 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL343105 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL441095 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL138873 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL138821 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL343712 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL138462 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL139438 | — | Ki | = | 57.0 | nM | 7.24 |