Assay Detail
Binding
CHEMBL5442192
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: HTR2B - 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.
28
Total Activities
28
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 |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.35 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4743049 | — | — | 1 | 8.00 |
| CHEMBL1516474 | TEGASEROD MALEATE | 4.0 | 1 | 7.81 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 7.40 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | 2.0 | 1 | 7.37 |
| CHEMBL1256998 | — | — | 1 | 7.28 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 7.19 |
| CHEMBL531742 | — | — | 1 | 6.64 |
| CHEMBL3215877 | — | — | 1 | 6.60 |
| CHEMBL519240 | — | — | 1 | 6.55 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4.0 | 1 | 6.44 |
| CHEMBL1836317 | — | — | 1 | 6.40 |
| CHEMBL59898 | — | — | 1 | 6.30 |
| CHEMBL214957 | — | — | 1 | 6.28 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 6.22 |
| CHEMBL259656 | — | — | 1 | 6.22 |
| CHEMBL3342358 | — | — | 1 | 6.19 |
| CHEMBL1436386 | — | — | 1 | 6.18 |
| CHEMBL542139 | — | — | 1 | 6.09 |
| CHEMBL34730 | — | — | 1 | 6.07 |
| CHEMBL1215661 | PRUVANSERIN | 2.0 | 1 | 5.98 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 5.94 |
| CHEMBL1334465 | — | — | 1 | 5.77 |
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 5.68 |
| CHEMBL3086703 | — | — | 1 | 5.61 |
| CHEMBL15766 | LY-255283 | — | 1 | 5.57 |
| CHEMBL2110363 | — | — | 1 | 5.52 |
| CHEMBL21283 | — | — | 1 | 5.36 |
| CHEMBL9387 | L-365260 | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4743049 | — | Ki | = | 9.943 | nM | 8.00 |
| CHEMBL1516474 | TEGASEROD MALEATE | Ki | = | 15.62 | nM | 7.81 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | Ki | = | 39.66 | nM | 7.40 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | Ki | = | 42.95 | nM | 7.37 |
| CHEMBL1256998 | — | Ki | = | 52.01 | nM | 7.28 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 65.01 | nM | 7.19 |
| CHEMBL531742 | — | Ki | = | 226.94 | nM | 6.64 |
| CHEMBL3215877 | — | Ki | = | 250.88 | nM | 6.60 |
| CHEMBL519240 | — | Ki | = | 279.58 | nM | 6.55 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | Ki | = | 362.25 | nM | 6.44 |
| CHEMBL1836317 | — | Ki | = | 400.17 | nM | 6.40 |
| CHEMBL59898 | — | Ki | = | 500.15 | nM | 6.30 |
| CHEMBL214957 | — | Ki | = | 527.78 | nM | 6.28 |
| CHEMBL589390 | LATREPIRDINE | Ki | = | 603.18 | nM | 6.22 |
| CHEMBL259656 | — | Ki | = | 607.3 | nM | 6.22 |
| CHEMBL3342358 | — | Ki | = | 646.69 | nM | 6.19 |
| CHEMBL1436386 | — | Ki | = | 656.45 | nM | 6.18 |
| CHEMBL542139 | — | Ki | = | 804.45 | nM | 6.09 |
| CHEMBL34730 | — | Ki | = | 844.11 | nM | 6.07 |
| CHEMBL1215661 | PRUVANSERIN | Ki | = | 1039.92 | nM | 5.98 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 1137.63 | nM | 5.94 |
| CHEMBL1334465 | — | Ki | = | 1700.78 | nM | 5.77 |
| CHEMBL24778 | SILODOSIN | Ki | = | 2091.7 | nM | 5.68 |
| CHEMBL3086703 | — | Ki | = | 2475.43 | nM | 5.61 |
| CHEMBL15766 | LY-255283 | Ki | = | 2684.72 | nM | 5.57 |
| CHEMBL2110363 | — | Ki | = | 3047.19 | nM | 5.52 |
| CHEMBL21283 | — | Ki | = | 4327.13 | nM | 5.36 |
| CHEMBL9387 | L-365260 | Ki | = | 6207.26 | nM | 5.21 |