Assay Detail
Binding
CHEMBL2026265
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Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.08 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1113 | AMOXAPINE | 4.0 | 1 | 8.75 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 8.62 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 8.31 |
| CHEMBL2022273 | — | — | 1 | 7.04 |
| CHEMBL716 | QUETIAPINE | 4.0 | 1 | 7.00 |
| CHEMBL2022269 | — | — | 1 | 6.88 |
| CHEMBL2022272 | — | — | 1 | 6.75 |
| CHEMBL2022280 | — | — | 1 | 6.69 |
| CHEMBL2022277 | — | — | 1 | 6.55 |
| CHEMBL2022276 | — | — | 1 | 6.45 |
| CHEMBL2022279 | — | — | 1 | 6.00 |
| CHEMBL2022271 | — | — | 1 | 5.96 |
| CHEMBL2022278 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1113 | AMOXAPINE | Ki | = | 1.77 | nM | 8.75 |
| CHEMBL831 | LOXAPINE | Ki | = | 2.42 | nM | 8.62 |
| CHEMBL42 | CLOZAPINE | Ki | = | 4.84 | nM | 8.31 |
| CHEMBL2022273 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL716 | QUETIAPINE | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL2022269 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL2022272 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL2022280 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL2022277 | — | Ki | = | 284.0 | nM | 6.55 |
| CHEMBL2022276 | — | Ki | = | 352.0 | nM | 6.45 |
| CHEMBL2022279 | — | Ki | = | 994.0 | nM | 6.00 |
| CHEMBL2022271 | — | Ki | = | 1106.0 | nM | 5.96 |
| CHEMBL2022278 | — | Ki | > | 1000.0 | nM | - |