Assay Detail
Binding
CHEMBL5442208
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PDSP Secondary Binding target: CHRM1 - 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.
16
Total Activities
16
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 | 16 | 6.34 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 8.36 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 8.06 |
| CHEMBL543113 | — | — | 1 | 8.01 |
| CHEMBL43383 | — | — | 1 | 6.59 |
| CHEMBL5076314 | — | — | 1 | 6.14 |
| CHEMBL18442 | PLERIXAFOR | 4.0 | 1 | 6.09 |
| CHEMBL2048820 | — | — | 1 | 6.07 |
| CHEMBL4743049 | — | — | 1 | 6.02 |
| CHEMBL1633 | KETOTIFEN FUMARATE | 4.0 | 1 | 5.98 |
| CHEMBL1474387 | — | — | 1 | 5.93 |
| CHEMBL214957 | — | — | 1 | 5.91 |
| CHEMBL281350 | SB-224289 | — | 1 | 5.90 |
| CHEMBL5089005 | — | — | 1 | 5.72 |
| CHEMBL531742 | — | — | 1 | 5.63 |
| CHEMBL103769 | — | — | 1 | 5.59 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | 4.0 | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 4.409 | nM | 8.36 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | Ki | = | 8.689 | nM | 8.06 |
| CHEMBL543113 | — | Ki | = | 9.74 | nM | 8.01 |
| CHEMBL43383 | — | Ki | = | 257.66 | nM | 6.59 |
| CHEMBL5076314 | — | Ki | = | 717.05 | nM | 6.14 |
| CHEMBL18442 | PLERIXAFOR | Ki | = | 803.62 | nM | 6.09 |
| CHEMBL2048820 | — | Ki | = | 846.35 | nM | 6.07 |
| CHEMBL4743049 | — | Ki | = | 955.21 | nM | 6.02 |
| CHEMBL1633 | KETOTIFEN FUMARATE | Ki | = | 1050.87 | nM | 5.98 |
| CHEMBL1474387 | — | Ki | = | 1183.45 | nM | 5.93 |
| CHEMBL214957 | — | Ki | = | 1237.37 | nM | 5.91 |
| CHEMBL281350 | SB-224289 | Ki | = | 1263.86 | nM | 5.90 |
| CHEMBL5089005 | — | Ki | = | 1909.85 | nM | 5.72 |
| CHEMBL531742 | — | Ki | = | 2331.58 | nM | 5.63 |
| CHEMBL103769 | — | Ki | = | 2577.5 | nM | 5.59 |
| CHEMBL1200809 | AZELASTINE HYDROCHLORIDE | Ki | = | 4277.1 | nM | 5.37 |