Assay Detail
Binding
CHEMBL4186929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta scintillation counting analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-HT1A and 5-HT2A receptors affinity, docking studies and pharmacological evaluation of a series of 8-acetyl-7-hydroxy-4-methylcoumarin derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.60 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 8.70 |
| CHEMBL4215550 | — | — | 1 | 8.22 |
| CHEMBL4214598 | — | — | 1 | 8.19 |
| CHEMBL4218720 | — | — | 1 | 8.15 |
| CHEMBL4215022 | — | — | 1 | 8.10 |
| CHEMBL4207177 | — | — | 1 | 8.00 |
| CHEMBL4213170 | — | — | 1 | 7.90 |
| CHEMBL4217736 | — | — | 1 | 7.70 |
| CHEMBL4207990 | — | — | 1 | 7.70 |
| CHEMBL4209403 | — | — | 1 | 7.66 |
| CHEMBL4212058 | — | — | 1 | 7.33 |
| CHEMBL4207585 | — | — | 1 | 7.31 |
| CHEMBL4218830 | — | — | 1 | 7.25 |
| CHEMBL4202831 | — | — | 1 | 7.24 |
| CHEMBL4213789 | — | — | 1 | 6.99 |
| CHEMBL4212943 | — | — | 1 | 6.40 |
| CHEMBL4210596 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6437 | MIANSERIN | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4215550 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4214598 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4218720 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4215022 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4207177 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4213170 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL4217736 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4207990 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4209403 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4212058 | — | Ki | = | 46.8 | nM | 7.33 |
| CHEMBL4207585 | — | Ki | = | 48.7 | nM | 7.31 |
| CHEMBL4218830 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL4202831 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4213789 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL4212943 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL4210596 | — | Ki | = | 408.0 | nM | 6.39 |