Assay Detail
Binding
CHEMBL5442201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: ADRA1D - 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.
26
Total Activities
26
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 | 26 | 6.12 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 7.33 |
| CHEMBL543113 | — | — | 1 | 7.24 |
| CHEMBL2105760 | BREXPIPRAZOLE | 4.0 | 1 | 7.12 |
| CHEMBL300555 | SPIROXATRINE | 2.0 | 1 | 6.86 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 6.49 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 6.48 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 6.42 |
| CHEMBL5087452 | — | — | 1 | 6.37 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.35 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | 4.0 | 1 | 6.14 |
| CHEMBL1095777 | INDACATEROL | 4.0 | 1 | 6.14 |
| CHEMBL589390 | LATREPIRDINE | 3.0 | 1 | 6.12 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.02 |
| CHEMBL1516474 | TEGASEROD MALEATE | 4.0 | 1 | 5.79 |
| CHEMBL1766103 | — | — | 1 | 5.78 |
| CHEMBL103769 | — | — | 1 | 5.77 |
| CHEMBL5076314 | — | — | 1 | 5.76 |
| CHEMBL1705 | CLONIDINE HYDROCHLORIDE | 4.0 | 1 | 5.70 |
| CHEMBL1235246 | — | — | 1 | 5.69 |
| CHEMBL2062257 | — | — | 1 | 5.68 |
| CHEMBL531742 | — | — | 1 | 5.68 |
| CHEMBL281350 | SB-224289 | — | 1 | 5.68 |
| CHEMBL214957 | — | — | 1 | 5.22 |
| CHEMBL519240 | — | — | 1 | 5.09 |
| CHEMBL260933 | GS 6201 | 1.0 | 1 | - |
| CHEMBL593013 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24778 | SILODOSIN | Ki | = | 47.32 | nM | 7.33 |
| CHEMBL543113 | — | Ki | = | 58.21 | nM | 7.24 |
| CHEMBL2105760 | BREXPIPRAZOLE | Ki | = | 76.44 | nM | 7.12 |
| CHEMBL300555 | SPIROXATRINE | Ki | = | 138.71 | nM | 6.86 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 333.27 | nM | 6.48 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 382.04 | nM | 6.42 |
| CHEMBL5087452 | — | Ki | = | 425.11 | nM | 6.37 |
| CHEMBL1200492 | NEFAZODONE HYDROCHLORIDE | Ki | = | 445.25 | nM | 6.35 |
| CHEMBL1615374 | VILAZODONE HYDROCHLORIDE | Ki | = | 716.31 | nM | 6.14 |
| CHEMBL1095777 | INDACATEROL | Ki | = | 731.31 | nM | 6.14 |
| CHEMBL589390 | LATREPIRDINE | Ki | = | 767.24 | nM | 6.12 |
| CHEMBL1263 | SALMETEROL | Ki | = | 963.16 | nM | 6.02 |
| CHEMBL1516474 | TEGASEROD MALEATE | Ki | = | 1638.89 | nM | 5.79 |
| CHEMBL1766103 | — | Ki | = | 1676.29 | nM | 5.78 |
| CHEMBL103769 | — | Ki | = | 1703.33 | nM | 5.77 |
| CHEMBL5076314 | — | Ki | = | 1749.45 | nM | 5.76 |
| CHEMBL1705 | CLONIDINE HYDROCHLORIDE | Ki | = | 1979.25 | nM | 5.70 |
| CHEMBL1235246 | — | Ki | = | 2054.47 | nM | 5.69 |
| CHEMBL2062257 | — | Ki | = | 2105.23 | nM | 5.68 |
| CHEMBL531742 | — | Ki | = | 2083.53 | nM | 5.68 |
| CHEMBL281350 | SB-224289 | Ki | = | 2106.2 | nM | 5.68 |
| CHEMBL214957 | — | Ki | = | 6052.02 | nM | 5.22 |
| CHEMBL519240 | — | Ki | = | 8031.56 | nM | 5.09 |
| CHEMBL260933 | GS 6201 | Ki | > | 10000.0 | nM | - |
| CHEMBL593013 | — | Ki | > | 10000.0 | nM | - |