Assay Detail
Binding
CHEMBL892801
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Displacement of [3H]ketanserin from serotonin 5HT2A receptor in rat brain cortex
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.93 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL390037 | — | — | 1 | 8.38 |
| CHEMBL408589 | — | — | 1 | 8.19 |
| CHEMBL231825 | — | — | 1 | 7.60 |
| CHEMBL232247 | — | — | 1 | 7.46 |
| CHEMBL398209 | — | — | 1 | 7.33 |
| CHEMBL209007 | — | — | 1 | 7.33 |
| CHEMBL390659 | — | — | 1 | 7.16 |
| CHEMBL398181 | — | — | 1 | 6.92 |
| CHEMBL232449 | — | — | 1 | 6.85 |
| CHEMBL208905 | — | — | 1 | 6.76 |
| CHEMBL378298 | — | — | 1 | 6.74 |
| CHEMBL232246 | — | — | 1 | 6.30 |
| CHEMBL232036 | — | — | 1 | 6.26 |
| CHEMBL232035 | — | — | 1 | 6.00 |
| CHEMBL279841 | — | — | 1 | 5.82 |
| CHEMBL207493 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL390037 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL408589 | — | Ki | = | 6.51 | nM | 8.19 |
| CHEMBL231825 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL232247 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL398209 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL209007 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL390659 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL398181 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL232449 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL208905 | — | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL378298 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL232246 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL232036 | — | Ki | = | 547.0 | nM | 6.26 |
| CHEMBL232035 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL279841 | — | Ki | = | 1510.0 | nM | 5.82 |
| CHEMBL207493 | — | Ki | = | 1510.0 | nM | 5.82 |