Assay Detail
Binding
CHEMBL4819277
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Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chlorine substituents and linker topology as factors of 5-HT<sub>6</sub>R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.49 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | 8.05 |
| CHEMBL4864863 | — | — | 1 | 6.99 |
| CHEMBL4860006 | — | — | 1 | 6.80 |
| CHEMBL4860719 | — | — | 1 | 6.69 |
| CHEMBL4858771 | — | — | 1 | 6.64 |
| CHEMBL4849077 | — | — | 1 | 6.57 |
| CHEMBL4860275 | — | — | 1 | 6.50 |
| CHEMBL4868911 | — | — | 1 | 6.45 |
| CHEMBL4876727 | — | — | 1 | 6.43 |
| CHEMBL4846146 | — | — | 1 | 6.43 |
| CHEMBL4864448 | — | — | 1 | 6.42 |
| CHEMBL4873623 | — | — | 1 | 6.38 |
| CHEMBL4849230 | — | — | 1 | 6.38 |
| CHEMBL4855393 | — | — | 1 | 6.37 |
| CHEMBL4873127 | — | — | 1 | 6.30 |
| CHEMBL4869411 | — | — | 1 | 6.30 |
| CHEMBL4857676 | — | — | 1 | 6.24 |
| CHEMBL4861431 | — | — | 1 | 6.12 |
| CHEMBL4447416 | — | — | 1 | 6.00 |
| CHEMBL4847379 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL715 | OLANZAPINE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4864863 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL4860006 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4860719 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL4858771 | — | Ki | = | 229.0 | nM | 6.64 |
| CHEMBL4849077 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL4860275 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL4868911 | — | Ki | = | 356.0 | nM | 6.45 |
| CHEMBL4876727 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL4846146 | — | Ki | = | 375.0 | nM | 6.43 |
| CHEMBL4864448 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL4873623 | — | Ki | = | 421.0 | nM | 6.38 |
| CHEMBL4849230 | — | Ki | = | 413.0 | nM | 6.38 |
| CHEMBL4855393 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL4873127 | — | Ki | = | 506.0 | nM | 6.30 |
| CHEMBL4869411 | — | Ki | = | 495.0 | nM | 6.30 |
| CHEMBL4857676 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL4861431 | — | Ki | = | 754.0 | nM | 6.12 |
| CHEMBL4447416 | — | Ki | = | 1001.0 | nM | 6.00 |
| CHEMBL4847379 | — | Ki | = | 1506.0 | nM | 5.82 |