Assay Detail
Binding
CHEMBL5442183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: SLC6A2 - 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.
43
Total Activities
43
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 noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 5.88 | 7.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 7.81 |
| CHEMBL1489369 | — | — | 1 | 7.02 |
| CHEMBL5076314 | — | — | 1 | 6.92 |
| CHEMBL3545036 | RASEGLURANT | 2.0 | 1 | 6.46 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.42 |
| CHEMBL1095777 | INDACATEROL | 4.0 | 1 | 6.25 |
| CHEMBL103769 | — | — | 1 | 6.21 |
| CHEMBL5089005 | — | — | 1 | 6.18 |
| CHEMBL267777 | RITANSERIN | 2.0 | 1 | 6.16 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 6.16 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.14 |
| CHEMBL543113 | — | — | 1 | 6.11 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.07 |
| CHEMBL1474387 | — | — | 1 | 6.02 |
| CHEMBL1256876 | — | — | 1 | 6.02 |
| CHEMBL567303 | PALOSURAN | 2.0 | 1 | 5.96 |
| CHEMBL5075931 | — | — | 1 | 5.90 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 5.84 |
| CHEMBL445102 | — | — | 1 | 5.83 |
| CHEMBL540612 | — | — | 1 | 5.78 |
| CHEMBL281350 | SB-224289 | — | 1 | 5.76 |
| CHEMBL4743495 | — | — | 1 | 5.73 |
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | 4.0 | 1 | 5.72 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | 2.0 | 1 | 5.71 |
| CHEMBL259656 | — | — | 1 | 5.60 |
| CHEMBL1215661 | PRUVANSERIN | 2.0 | 1 | 5.60 |
| CHEMBL1376064 | — | — | 1 | 5.59 |
| CHEMBL1256863 | — | — | 1 | 5.58 |
| CHEMBL300555 | SPIROXATRINE | 2.0 | 1 | 5.58 |
| CHEMBL59898 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 15.48 | nM | 7.81 |
| CHEMBL1489369 | — | Ki | = | 96.28 | nM | 7.02 |
| CHEMBL5076314 | — | Ki | = | 119.74 | nM | 6.92 |
| CHEMBL3545036 | RASEGLURANT | Ki | = | 344.55 | nM | 6.46 |
| CHEMBL1263 | SALMETEROL | Ki | = | 381.86 | nM | 6.42 |
| CHEMBL1095777 | INDACATEROL | Ki | = | 568.66 | nM | 6.25 |
| CHEMBL103769 | — | Ki | = | 618.45 | nM | 6.21 |
| CHEMBL5089005 | — | Ki | = | 664.12 | nM | 6.18 |
| CHEMBL267777 | RITANSERIN | Ki | = | 685.41 | nM | 6.16 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 689.21 | nM | 6.16 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 730.55 | nM | 6.14 |
| CHEMBL543113 | — | Ki | = | 768.78 | nM | 6.11 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 857.24 | nM | 6.07 |
| CHEMBL1474387 | — | Ki | = | 955.76 | nM | 6.02 |
| CHEMBL1256876 | — | Ki | = | 951.15 | nM | 6.02 |
| CHEMBL567303 | PALOSURAN | Ki | = | 1087.42 | nM | 5.96 |
| CHEMBL5075931 | — | Ki | = | 1257.91 | nM | 5.90 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | Ki | = | 1451.11 | nM | 5.84 |
| CHEMBL445102 | — | Ki | = | 1474.18 | nM | 5.83 |
| CHEMBL540612 | — | Ki | = | 1672.83 | nM | 5.78 |
| CHEMBL281350 | SB-224289 | Ki | = | 1729.62 | nM | 5.76 |
| CHEMBL4743495 | — | Ki | = | 1851.4 | nM | 5.73 |
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | Ki | = | 1919.11 | nM | 5.72 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | Ki | = | 1926.42 | nM | 5.71 |
| CHEMBL259656 | — | Ki | = | 2537.76 | nM | 5.60 |
| CHEMBL1215661 | PRUVANSERIN | Ki | = | 2517.97 | nM | 5.60 |
| CHEMBL1376064 | — | Ki | = | 2583.75 | nM | 5.59 |
| CHEMBL1256863 | — | Ki | = | 2646.67 | nM | 5.58 |
| CHEMBL300555 | SPIROXATRINE | Ki | = | 2610.05 | nM | 5.58 |
| CHEMBL59898 | — | Ki | = | 2850.37 | nM | 5.54 |
| CHEMBL21283 | — | Ki | = | 3223.29 | nM | 5.49 |
| CHEMBL2106195 | DEXMEDETOMIDINE HYDROCHLORIDE | Ki | = | 3261.37 | nM | 5.49 |
| CHEMBL23327 | PURVALANOLA | Ki | = | 4399.46 | nM | 5.36 |
| CHEMBL2103873 | MACITENTAN | Ki | = | 4831.14 | nM | 5.32 |
| CHEMBL542139 | — | Ki | = | 5615.65 | nM | 5.25 |
| CHEMBL1766103 | — | Ki | = | 5806.31 | nM | 5.24 |
| CHEMBL7353 | — | Ki | = | 6905.57 | nM | 5.16 |
| CHEMBL143210 | — | Ki | = | 7552.66 | nM | 5.12 |
| CHEMBL2181226 | — | Ki | = | 7741.05 | nM | 5.11 |
| CHEMBL403225 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL502882 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2057618 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL83894 | FANANSERIN | Ki | > | 10000.0 | nM | - |