Assay Detail
Binding
CHEMBL3243815
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125]DOI from human recombinant full length 5HT2C receptor expressed in HEK293E cells
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293E |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 6.52 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.15 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 7.89 |
| CHEMBL3233427 | — | — | 1 | 7.08 |
| CHEMBL3233406 | — | — | 1 | 7.05 |
| CHEMBL3233428 | — | — | 1 | 6.96 |
| CHEMBL3233431 | — | — | 1 | 6.82 |
| CHEMBL3233142 | LUMATEPERONE TOSYLATE | 4.0 | 1 | 6.76 |
| CHEMBL3233430 | — | — | 1 | 6.71 |
| CHEMBL3233146 | — | — | 1 | 6.62 |
| CHEMBL3233409 | — | — | 1 | 6.59 |
| CHEMBL3233143 | — | — | 1 | 6.55 |
| CHEMBL3233425 | — | — | 1 | 6.55 |
| CHEMBL3233411 | — | — | 1 | 6.54 |
| CHEMBL3233144 | — | — | 1 | 6.54 |
| CHEMBL3233412 | — | — | 1 | 6.52 |
| CHEMBL3233147 | — | — | 1 | 6.42 |
| CHEMBL3233145 | — | — | 1 | 6.30 |
| CHEMBL3233423 | — | — | 1 | 6.30 |
| CHEMBL3233429 | — | — | 1 | 6.29 |
| CHEMBL3233432 | — | — | 1 | 6.28 |
| CHEMBL3233419 | — | — | 1 | 6.27 |
| CHEMBL3233148 | — | — | 1 | 6.24 |
| CHEMBL3233433 | — | — | 1 | 6.19 |
| CHEMBL3233422 | — | — | 1 | 6.15 |
| CHEMBL3233426 | — | — | 1 | 6.06 |
| CHEMBL3233407 | — | — | 1 | 5.96 |
| CHEMBL3233149 | — | — | 1 | 5.96 |
| CHEMBL3233424 | — | — | 1 | 5.89 |
| CHEMBL3233414 | — | — | 1 | 5.48 |
| CHEMBL3233421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL42 | CLOZAPINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3233427 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL3233406 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL3233428 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL3233431 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3233142 | LUMATEPERONE TOSYLATE | Ki | = | 173.0 | nM | 6.76 |
| CHEMBL3233430 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL3233146 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL3233409 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL3233425 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL3233143 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL3233411 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL3233144 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL3233412 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3233147 | — | Ki | = | 385.0 | nM | 6.42 |
| CHEMBL3233145 | — | Ki | = | 498.0 | nM | 6.30 |
| CHEMBL3233423 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL3233429 | — | Ki | = | 507.0 | nM | 6.29 |
| CHEMBL3233432 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL3233419 | — | Ki | = | 532.0 | nM | 6.27 |
| CHEMBL3233148 | — | Ki | = | 582.0 | nM | 6.24 |
| CHEMBL3233433 | — | Ki | = | 641.0 | nM | 6.19 |
| CHEMBL3233422 | — | Ki | = | 702.0 | nM | 6.15 |
| CHEMBL3233426 | — | Ki | = | 862.0 | nM | 6.06 |
| CHEMBL3233407 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL3233149 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL3233424 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL3233414 | — | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL3233408 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3233410 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3233413 | — | Ki | - | — | - | |
| CHEMBL3233415 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3233416 | — | Ki | - | — | - | |
| CHEMBL3233417 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3233418 | — | Ki | - | — | - | |
| CHEMBL3233420 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3233421 | — | Ki | > | 1000.0 | nM | - |