Assay Detail
Binding
CHEMBL617506
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Displacement of [3H]mesulergine from 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.38 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14563 | SB-242084 | — | 1 | 9.00 |
| CHEMBL276140 | — | — | 1 | 8.60 |
| CHEMBL42024 | — | — | 1 | 8.20 |
| CHEMBL265991 | — | — | 1 | 8.20 |
| CHEMBL297784 | — | — | 1 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14563 | SB-242084 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL276140 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL42024 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL265991 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL297784 | — | Ki | = | 12.59 | nM | 7.90 |