Assay Detail
Binding
CHEMBL617459
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Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.37 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.11 |
| CHEMBL72292 | — | — | 1 | 8.10 |
| CHEMBL415300 | ISOCLOZAPINE | — | 1 | 7.92 |
| CHEMBL72794 | — | — | 1 | 7.92 |
| CHEMBL308090 | — | — | 1 | 7.46 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.26 |
| CHEMBL73074 | — | — | 1 | 6.80 |
| CHEMBL70377 | — | — | 1 | 6.51 |
| CHEMBL310712 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42 | CLOZAPINE | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL72292 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL415300 | ISOCLOZAPINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL72794 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL308090 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL73074 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL70377 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL310712 | — | IC50 | = | 550.0 | nM | 6.26 |