Assay Detail
Binding
CHEMBL828759
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Binding affinity toward 5-HT2C receptor evaluated by displacement of [3H]5-HT radioligand
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.13 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL190699 | — | — | 1 | 9.52 |
| CHEMBL190124 | — | — | 1 | 8.89 |
| CHEMBL361079 | — | — | 1 | 8.85 |
| CHEMBL187739 | — | — | 1 | 8.82 |
| CHEMBL188033 | — | — | 1 | 8.77 |
| CHEMBL191054 | — | — | 1 | 8.72 |
| CHEMBL2112055 | — | — | 1 | 8.66 |
| CHEMBL190584 | — | — | 1 | 8.59 |
| CHEMBL187888 | — | — | 1 | 8.42 |
| CHEMBL364534 | — | — | 1 | 8.02 |
| CHEMBL2096809 | — | — | 2 | 7.89 |
| CHEMBL188605 | — | — | 1 | 7.51 |
| CHEMBL425545 | — | — | 1 | 7.50 |
| CHEMBL361929 | — | — | 1 | 7.47 |
| CHEMBL2096711 | — | — | 1 | 6.75 |
| CHEMBL187787 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL190699 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL190124 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL361079 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL187739 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL188033 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL191054 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2112055 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL190584 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL187888 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL364534 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL2096809 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2096809 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL188605 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL425545 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL361929 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2096711 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL187787 | — | Ki | = | 680.0 | nM | 6.17 |