Assay Detail
Binding
CHEMBL5442209
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PDSP Secondary Binding target: CHRM2 - 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.
15
Total Activities
15
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 | 15 | 6.54 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.15 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 7.88 |
| CHEMBL43383 | — | — | 1 | 7.84 |
| CHEMBL5076314 | — | — | 1 | 6.69 |
| CHEMBL2048820 | — | — | 1 | 6.62 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 6.61 |
| CHEMBL2018875 | — | — | 1 | 6.28 |
| CHEMBL5089005 | — | — | 1 | 6.19 |
| CHEMBL1474387 | — | — | 1 | 6.09 |
| CHEMBL18442 | PLERIXAFOR | 4.0 | 1 | 5.99 |
| CHEMBL360648 | — | — | 1 | 5.46 |
| CHEMBL2431212 | — | — | 1 | 5.17 |
| CHEMBL2419490 | — | — | 1 | 5.04 |
| CHEMBL1334465 | — | — | 1 | - |
| CHEMBL2110363 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.7036 | nM | 9.15 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | Ki | = | 13.12 | nM | 7.88 |
| CHEMBL43383 | — | Ki | = | 14.46 | nM | 7.84 |
| CHEMBL5076314 | — | Ki | = | 203.56 | nM | 6.69 |
| CHEMBL2048820 | — | Ki | = | 242.85 | nM | 6.62 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 243.81 | nM | 6.61 |
| CHEMBL2018875 | — | Ki | = | 527.84 | nM | 6.28 |
| CHEMBL5089005 | — | Ki | = | 640.77 | nM | 6.19 |
| CHEMBL1474387 | — | Ki | = | 804.92 | nM | 6.09 |
| CHEMBL18442 | PLERIXAFOR | Ki | = | 1013.99 | nM | 5.99 |
| CHEMBL360648 | — | Ki | = | 3436.77 | nM | 5.46 |
| CHEMBL2431212 | — | Ki | = | 6746.06 | nM | 5.17 |
| CHEMBL2419490 | — | Ki | = | 9065.67 | nM | 5.04 |
| CHEMBL1334465 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2110363 | — | Ki | > | 10000.0 | nM | - |