Assay Detail
Binding
CHEMBL5442211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: CHRM4 - 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.
13
Total Activities
13
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 M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
EUbOPEN Chemogenomics Library - PDSP Secondary Binding
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.66 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.22 |
| CHEMBL43383 | — | — | 1 | 7.87 |
| CHEMBL59898 | — | — | 1 | 7.33 |
| CHEMBL2048820 | — | — | 1 | 6.74 |
| CHEMBL360648 | — | — | 1 | 6.60 |
| CHEMBL4743049 | — | — | 1 | 6.35 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | 4.0 | 1 | 6.11 |
| CHEMBL1474387 | — | — | 1 | 6.07 |
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | 4.0 | 1 | 6.05 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 6.04 |
| CHEMBL214957 | — | — | 1 | 5.77 |
| CHEMBL531742 | — | — | 1 | 5.71 |
| CHEMBL23327 | PURVALANOLA | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL43383 | — | Ki | = | 13.59 | nM | 7.87 |
| CHEMBL59898 | — | Ki | = | 46.93 | nM | 7.33 |
| CHEMBL2048820 | — | Ki | = | 181.09 | nM | 6.74 |
| CHEMBL360648 | — | Ki | = | 248.86 | nM | 6.60 |
| CHEMBL4743049 | — | Ki | = | 443.96 | nM | 6.35 |
| CHEMBL2024517 | CARIPRAZINE HYDROCHLORIDE | Ki | = | 778.76 | nM | 6.11 |
| CHEMBL1474387 | — | Ki | = | 854.47 | nM | 6.07 |
| CHEMBL4164059 | PITOLISANT HYDROCHLORIDE | Ki | = | 899.29 | nM | 6.05 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 917.28 | nM | 6.04 |
| CHEMBL214957 | — | Ki | = | 1703.92 | nM | 5.77 |
| CHEMBL531742 | — | Ki | = | 1958.4 | nM | 5.71 |
| CHEMBL23327 | PURVALANOLA | Ki | > | 10000.0 | nM | - |