Assay Detail
Binding
CHEMBL5442176
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: CHRM5 - 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.
30
Total Activities
30
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
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.14 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 8.91 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 8.41 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 7.01 |
| CHEMBL4743049 | — | — | 1 | 6.53 |
| CHEMBL2164327 | — | — | 1 | 6.51 |
| CHEMBL281350 | SB-224289 | — | 1 | 6.46 |
| CHEMBL360648 | — | — | 1 | 6.33 |
| CHEMBL103769 | — | — | 1 | 6.31 |
| CHEMBL1474387 | — | — | 1 | 6.29 |
| CHEMBL445102 | — | — | 1 | 6.24 |
| CHEMBL3039520 | LASMIDITAN | 4.0 | 1 | 6.20 |
| CHEMBL2048820 | — | — | 1 | 6.18 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 6.14 |
| CHEMBL2018875 | — | — | 1 | 6.08 |
| CHEMBL43383 | — | — | 1 | 6.03 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.01 |
| CHEMBL2181226 | — | — | 1 | 5.90 |
| CHEMBL79834 | SPIRAMIDE | 2.0 | 1 | 5.88 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 5.84 |
| CHEMBL4743495 | — | — | 1 | 5.66 |
| CHEMBL214957 | — | — | 1 | 5.58 |
| CHEMBL16192 | CP-96345 | — | 1 | 5.31 |
| CHEMBL2392141 | — | — | 1 | 5.28 |
| CHEMBL1256750 | — | — | 1 | 5.23 |
| CHEMBL3310783 | — | — | 1 | 5.18 |
| CHEMBL3287574 | — | — | 1 | 5.16 |
| CHEMBL2381848 | PF-06291874 | 2.0 | 1 | 5.07 |
| CHEMBL2440659 | — | — | 1 | - |
| CHEMBL2435402 | — | — | 1 | - |
| CHEMBL2182029 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 1.22 | nM | 8.91 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | Ki | = | 3.864 | nM | 8.41 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 98.53 | nM | 7.01 |
| CHEMBL4743049 | — | Ki | = | 293.13 | nM | 6.53 |
| CHEMBL2164327 | — | Ki | = | 308.28 | nM | 6.51 |
| CHEMBL281350 | SB-224289 | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL360648 | — | Ki | = | 467.2 | nM | 6.33 |
| CHEMBL103769 | — | Ki | = | 490.8 | nM | 6.31 |
| CHEMBL1474387 | — | Ki | = | 510.27 | nM | 6.29 |
| CHEMBL445102 | — | Ki | = | 579.3 | nM | 6.24 |
| CHEMBL3039520 | LASMIDITAN | Ki | = | 632.05 | nM | 6.20 |
| CHEMBL2048820 | — | Ki | = | 662.06 | nM | 6.18 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 717.63 | nM | 6.14 |
| CHEMBL2018875 | — | Ki | = | 840.81 | nM | 6.08 |
| CHEMBL43383 | — | Ki | = | 944.28 | nM | 6.03 |
| CHEMBL1263 | SALMETEROL | Ki | = | 971.3 | nM | 6.01 |
| CHEMBL2181226 | — | Ki | = | 1249.97 | nM | 5.90 |
| CHEMBL79834 | SPIRAMIDE | Ki | = | 1310.54 | nM | 5.88 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 1432.02 | nM | 5.84 |
| CHEMBL4743495 | — | Ki | = | 2191.04 | nM | 5.66 |
| CHEMBL214957 | — | Ki | = | 2641.8 | nM | 5.58 |
| CHEMBL16192 | CP-96345 | Ki | = | 4935.15 | nM | 5.31 |
| CHEMBL2392141 | — | Ki | = | 5234.8 | nM | 5.28 |
| CHEMBL1256750 | — | Ki | = | 5914.25 | nM | 5.23 |
| CHEMBL3310783 | — | Ki | = | 6559.94 | nM | 5.18 |
| CHEMBL3287574 | — | Ki | = | 6848.57 | nM | 5.16 |
| CHEMBL2381848 | PF-06291874 | Ki | = | 8582.23 | nM | 5.07 |
| CHEMBL2440659 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2435402 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2182029 | — | Ki | > | 10000.0 | nM | - |