Assay Detail
Binding
CHEMBL4366764
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Displacement of [3H]-8-OH-DPAT from human 5-HT1A expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay
19
Total Activities
19
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
Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT<sub>6</sub>.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.38 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.70 |
| CHEMBL4473083 | — | — | 1 | 5.79 |
| CHEMBL4591878 | — | — | 1 | 5.78 |
| CHEMBL4580959 | — | — | 1 | 5.50 |
| CHEMBL4515075 | — | — | 1 | 5.47 |
| CHEMBL4522568 | — | — | 1 | 5.46 |
| CHEMBL4527124 | — | — | 1 | 5.45 |
| CHEMBL4557247 | — | — | 1 | 5.36 |
| CHEMBL4447416 | — | — | 1 | 5.34 |
| CHEMBL4462404 | — | — | 1 | 5.28 |
| CHEMBL4548041 | — | — | 1 | 5.26 |
| CHEMBL4524981 | — | — | 1 | 5.12 |
| CHEMBL4560883 | — | — | 1 | 5.11 |
| CHEMBL4465929 | — | — | 1 | 5.06 |
| CHEMBL4520796 | — | — | 1 | 4.90 |
| CHEMBL4570584 | — | — | 1 | 4.85 |
| CHEMBL4532712 | — | — | 1 | 4.82 |
| CHEMBL4584325 | — | — | 1 | 4.54 |
| CHEMBL4441655 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4473083 | — | Ki | = | 1610.0 | nM | 5.79 |
| CHEMBL4591878 | — | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL4580959 | — | Ki | = | 3176.0 | nM | 5.50 |
| CHEMBL4515075 | — | Ki | = | 3384.0 | nM | 5.47 |
| CHEMBL4522568 | — | Ki | = | 3438.0 | nM | 5.46 |
| CHEMBL4527124 | — | Ki | = | 3584.0 | nM | 5.45 |
| CHEMBL4557247 | — | Ki | = | 4389.0 | nM | 5.36 |
| CHEMBL4447416 | — | Ki | = | 4540.0 | nM | 5.34 |
| CHEMBL4462404 | — | Ki | = | 5311.0 | nM | 5.28 |
| CHEMBL4548041 | — | Ki | = | 5467.0 | nM | 5.26 |
| CHEMBL4524981 | — | Ki | = | 7505.0 | nM | 5.12 |
| CHEMBL4560883 | — | Ki | = | 7688.0 | nM | 5.11 |
| CHEMBL4465929 | — | Ki | = | 8726.0 | nM | 5.06 |
| CHEMBL4520796 | — | Ki | = | 12530.0 | nM | 4.90 |
| CHEMBL4570584 | — | Ki | = | 14160.0 | nM | 4.85 |
| CHEMBL4532712 | — | Ki | = | 15070.0 | nM | 4.82 |
| CHEMBL4584325 | — | Ki | = | 28510.0 | nM | 4.54 |
| CHEMBL4441655 | — | Ki | > | 1000000.0 | nM | - |