Assay Detail
Functional
CHEMBL4368231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5HT2A receptor expressed in CHOK1 cells assessed as inhibition of 5-HT induced inositol phosphate production incubated for 24 hrs followed by 5-HT addition by HTRF assay
10
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.36 | 9.15 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 9.15 |
| CHEMBL4554558 | — | — | 2 | 5.62 |
| CHEMBL285157 | — | — | 2 | 5.58 |
| CHEMBL4552542 | — | — | 2 | 5.10 |
| CHEMBL18840 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85 | RISPERIDONE | IC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4554558 | — | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL4554558 | — | IC50 | = | 2415.0 | nM | 5.62 |
| CHEMBL285157 | — | IC50 | = | 2630.27 | nM | 5.58 |
| CHEMBL285157 | — | IC50 | = | 2618.0 | nM | 5.58 |
| CHEMBL4552542 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4552542 | — | IC50 | = | 7980.0 | nM | 5.10 |
| CHEMBL18840 | — | IC50 | - | — | - | |
| CHEMBL18840 | — | pIC50 | - | — | - |