Assay Detail
Binding
CHEMBL5442191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: SLC6A4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Category | PDSP assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 6.31 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 9.33 |
| CHEMBL1489369 | — | — | 1 | 7.76 |
| CHEMBL445102 | — | — | 1 | 7.53 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 7.18 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.76 |
| CHEMBL103769 | — | — | 1 | 6.68 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 6.68 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.53 |
| CHEMBL540612 | — | — | 1 | 6.52 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 6.29 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 6.25 |
| CHEMBL1095777 | INDACATEROL | 4.0 | 1 | 6.11 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 6.11 |
| CHEMBL5089005 | — | — | 1 | 6.08 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.06 |
| CHEMBL567303 | PALOSURAN | 2.0 | 1 | 6.00 |
| CHEMBL83894 | FANANSERIN | 2.0 | 1 | 5.96 |
| CHEMBL1215661 | PRUVANSERIN | 2.0 | 1 | 5.96 |
| CHEMBL5076314 | — | — | 1 | 5.94 |
| CHEMBL2057618 | — | — | 1 | 5.61 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 5.51 |
| CHEMBL1376064 | — | — | 1 | 5.39 |
| CHEMBL34730 | — | — | 1 | 5.36 |
| CHEMBL143210 | — | — | 1 | 5.12 |
| CHEMBL7353 | — | — | 1 | 5.11 |
| CHEMBL1256844 | — | — | 1 | - |
| CHEMBL2103873 | MACITENTAN | 4.0 | 1 | - |
| CHEMBL2062257 | — | — | 1 | - |
| CHEMBL679 | EPINEPHRINE | 4.0 | 1 | - |
| CHEMBL214957 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 0.4705 | nM | 9.33 |
| CHEMBL1489369 | — | Ki | = | 17.18 | nM | 7.76 |
| CHEMBL445102 | — | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 65.55 | nM | 7.18 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 175.27 | nM | 6.76 |
| CHEMBL103769 | — | Ki | = | 208.79 | nM | 6.68 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 210.16 | nM | 6.68 |
| CHEMBL1263 | SALMETEROL | Ki | = | 294.2 | nM | 6.53 |
| CHEMBL540612 | — | Ki | = | 303.88 | nM | 6.52 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | Ki | = | 517.19 | nM | 6.29 |
| CHEMBL267777 | RITANSERIN | Ki | = | 567.74 | nM | 6.25 |
| CHEMBL1095777 | INDACATEROL | Ki | = | 770.02 | nM | 6.11 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | Ki | = | 785.15 | nM | 6.11 |
| CHEMBL5089005 | — | Ki | = | 833.1 | nM | 6.08 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 862.09 | nM | 6.06 |
| CHEMBL567303 | PALOSURAN | Ki | = | 995.29 | nM | 6.00 |
| CHEMBL83894 | FANANSERIN | Ki | = | 1101.92 | nM | 5.96 |
| CHEMBL1215661 | PRUVANSERIN | Ki | = | 1100.27 | nM | 5.96 |
| CHEMBL5076314 | — | Ki | = | 1145.25 | nM | 5.94 |
| CHEMBL2057618 | — | Ki | = | 2433.32 | nM | 5.61 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 3076.1 | nM | 5.51 |
| CHEMBL1376064 | — | Ki | = | 4054.15 | nM | 5.39 |
| CHEMBL34730 | — | Ki | = | 4376.23 | nM | 5.36 |
| CHEMBL143210 | — | Ki | = | 7612.02 | nM | 5.12 |
| CHEMBL7353 | — | Ki | = | 7773.2 | nM | 5.11 |
| CHEMBL1256844 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2103873 | MACITENTAN | Ki | > | 10000.0 | nM | - |
| CHEMBL2062257 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL679 | EPINEPHRINE | Ki | > | 10000.0 | nM | - |
| CHEMBL214957 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL593013 | — | Ki | > | 10000.0 | nM | - |