Assay Detail
Binding
CHEMBL953250
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Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.31 | 9.80 |
| pKi | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31354 | WAY-100,635 | — | 1 | 9.80 |
| CHEMBL183460 | — | — | 1 | 9.50 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 9.10 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 8.90 |
| CHEMBL494806 | — | — | 1 | 8.70 |
| CHEMBL494991 | — | — | 1 | 8.30 |
| CHEMBL494992 | — | — | 1 | 7.90 |
| CHEMBL494631 | — | — | 1 | 7.60 |
| CHEMBL495160 | — | — | 1 | 6.80 |
| CHEMBL425190 | — | — | 1 | 6.50 |
| CHEMBL506942 | — | — | 1 | - |
| CHEMBL495161 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31354 | WAY-100,635 | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL183460 | — | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL39 | SEROTONIN | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL494806 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL494991 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL494992 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL494631 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL495160 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL425190 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL506942 | — | pKi | - | — | - | |
| CHEMBL495161 | — | pKi | - | — | - |