Assay Detail
Binding
CHEMBL954043
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Inhibition of [3H]5HT uptake at SERT in rat cortical synaptosomes
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.28 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183460 | — | — | 1 | 8.00 |
| CHEMBL498356 | — | — | 1 | 7.10 |
| CHEMBL495895 | — | — | 1 | 6.70 |
| CHEMBL525362 | — | — | 1 | 6.60 |
| CHEMBL425190 | — | — | 1 | 6.50 |
| CHEMBL494991 | — | — | 1 | 6.40 |
| CHEMBL496098 | — | — | 1 | 6.40 |
| CHEMBL495213 | — | — | 1 | 6.40 |
| CHEMBL525712 | — | — | 1 | 6.30 |
| CHEMBL498355 | — | — | 1 | 6.30 |
| CHEMBL494992 | — | — | 1 | 6.20 |
| CHEMBL495217 | — | — | 1 | 6.20 |
| CHEMBL522708 | — | — | 1 | 6.10 |
| CHEMBL494631 | — | — | 1 | 6.10 |
| CHEMBL497127 | — | — | 1 | 6.10 |
| CHEMBL498354 | — | — | 1 | 6.10 |
| CHEMBL495046 | — | — | 1 | 6.00 |
| CHEMBL497963 | — | — | 1 | 6.00 |
| CHEMBL506942 | — | — | 1 | 6.00 |
| CHEMBL494806 | — | — | 1 | 5.90 |
| CHEMBL495160 | — | — | 1 | 5.80 |
| CHEMBL495161 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183460 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL498356 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL495895 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL525362 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL425190 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL494991 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL496098 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL495213 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL525712 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL498355 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL494992 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL495217 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL522708 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL494631 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL497127 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL498354 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL495046 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL497963 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL506942 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL494806 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL495160 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL495161 | — | Ki | = | 10000.0 | nM | 5.00 |