Assay Detail
Functional
CHEMBL982072
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at peripheral muscarinic M4 receptor in rabbit vas deferens assessed as effect on McN-A-343-induced contraction after 1 hr
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Vas deferens |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| Kd | 8 | 8.09 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2021478 | — | — | 1 | 8.85 |
| CHEMBL2021479 | — | — | 1 | 8.72 |
| CHEMBL2021476 | — | — | 1 | 8.44 |
| CHEMBL2021477 | — | — | 1 | 8.38 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 8.05 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 7.95 |
| CHEMBL478227 | — | — | 1 | 7.22 |
| CHEMBL478226 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2021478 | — | Kd | = | 1.413 | nM | 8.85 |
| CHEMBL2021479 | — | Kd | = | 1.905 | nM | 8.72 |
| CHEMBL2021476 | — | Kd | = | 3.631 | nM | 8.44 |
| CHEMBL2021477 | — | Kd | = | 4.169 | nM | 8.38 |
| CHEMBL9967 | PIRENZEPINE | Kd | = | 8.913 | nM | 8.05 |
| CHEMBL265256 | TRIPITRAMINE | Kd | = | 11.22 | nM | 7.95 |
| CHEMBL478227 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL478226 | — | Kd | = | 79.43 | nM | 7.10 |