Assay Detail
Binding
CHEMBL982066
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M1 receptor expressed in CHOK1 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.45 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 8.55 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 8.45 |
| CHEMBL2021478 | — | — | 1 | 8.20 |
| CHEMBL2021479 | — | — | 1 | 7.90 |
| CHEMBL2021476 | — | — | 1 | 7.65 |
| CHEMBL2021477 | — | — | 1 | 7.34 |
| CHEMBL478227 | — | — | 1 | 5.84 |
| CHEMBL478226 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9967 | PIRENZEPINE | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL2021478 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL2021479 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL2021476 | — | Ki | = | 22.39 | nM | 7.65 |
| CHEMBL2021477 | — | Ki | = | 45.71 | nM | 7.34 |
| CHEMBL478227 | — | Ki | = | 1445.44 | nM | 5.84 |
| CHEMBL478226 | — | Ki | = | 2290.87 | nM | 5.64 |