Assay Detail
Binding
CHEMBL5442210
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: CHRM3 - 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.
14
Total Activities
14
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 | 14 | 6.63 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.48 |
| CHEMBL543113 | — | — | 1 | 8.23 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 7.86 |
| CHEMBL43383 | — | — | 1 | 6.82 |
| CHEMBL59898 | — | — | 1 | 6.76 |
| CHEMBL360648 | — | — | 1 | 6.15 |
| CHEMBL4743049 | — | — | 1 | 6.07 |
| CHEMBL281350 | SB-224289 | — | 1 | 6.03 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 6.00 |
| CHEMBL1474387 | — | — | 1 | 5.94 |
| CHEMBL2048820 | — | — | 1 | 5.82 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 5.67 |
| CHEMBL214957 | — | — | 1 | 5.38 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.3298 | nM | 9.48 |
| CHEMBL543113 | — | Ki | = | 5.82 | nM | 8.23 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | Ki | = | 13.75 | nM | 7.86 |
| CHEMBL43383 | — | Ki | = | 152.23 | nM | 6.82 |
| CHEMBL59898 | — | Ki | = | 172.9 | nM | 6.76 |
| CHEMBL360648 | — | Ki | = | 706.8 | nM | 6.15 |
| CHEMBL4743049 | — | Ki | = | 850.84 | nM | 6.07 |
| CHEMBL281350 | SB-224289 | Ki | = | 926.08 | nM | 6.03 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 995.75 | nM | 6.00 |
| CHEMBL1474387 | — | Ki | = | 1138.54 | nM | 5.94 |
| CHEMBL2048820 | — | Ki | = | 1527.21 | nM | 5.82 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 2148.08 | nM | 5.67 |
| CHEMBL214957 | — | Ki | = | 4131.43 | nM | 5.38 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | > | 10000.0 | nM | - |