Assay Detail
Binding
CHEMBL861243
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]5HT from human recombinant 5HT2B receptor expressed in CHO cells
18
Total Activities
18
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
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.73 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL190699 | — | — | 1 | 8.49 |
| CHEMBL191054 | — | — | 1 | 7.40 |
| CHEMBL203230 | — | — | 1 | 7.32 |
| CHEMBL206333 | — | — | 1 | 7.17 |
| CHEMBL206845 | — | — | 1 | 7.11 |
| CHEMBL203393 | — | — | 1 | 7.09 |
| CHEMBL383694 | — | — | 1 | 6.78 |
| CHEMBL203013 | — | — | 1 | 6.76 |
| CHEMBL203025 | — | — | 1 | 6.66 |
| CHEMBL203396 | — | — | 1 | 6.66 |
| CHEMBL206394 | — | — | 1 | 6.53 |
| CHEMBL383051 | — | — | 1 | 6.42 |
| CHEMBL205671 | — | — | 1 | 6.36 |
| CHEMBL382618 | — | — | 1 | 6.08 |
| CHEMBL206386 | — | — | 1 | 5.94 |
| CHEMBL206618 | — | — | 1 | 5.88 |
| CHEMBL202795 | — | — | 1 | 5.74 |
| CHEMBL382471 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL190699 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL191054 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL203230 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL206333 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL206845 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL203393 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL383694 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL203013 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL203025 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL203396 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL206394 | — | Ki | = | 295.0 | nM | 6.53 |
| CHEMBL383051 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL205671 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL382618 | — | Ki | = | 835.0 | nM | 6.08 |
| CHEMBL206386 | — | Ki | = | 1139.0 | nM | 5.94 |
| CHEMBL206618 | — | Ki | = | 1306.0 | nM | 5.88 |
| CHEMBL202795 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL382471 | — | Ki | - | — | - |