Assay Detail
Functional
CHEMBL982071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at peripheral muscarinic M3 receptor in guinea pig longitudinal ileum assessed as effect on arecaidin propargyl ester-induced contraction after 1 hr
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 | 7.06 | 7.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2021476 | — | — | 1 | 7.76 |
| CHEMBL2021479 | — | — | 1 | 7.64 |
| CHEMBL2021477 | — | — | 1 | 7.58 |
| CHEMBL2021478 | — | — | 1 | 7.57 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.88 |
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 6.55 |
| CHEMBL478226 | — | — | 1 | 6.47 |
| CHEMBL478227 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2021476 | — | Kd | = | 17.38 | nM | 7.76 |
| CHEMBL2021479 | — | Kd | = | 22.91 | nM | 7.64 |
| CHEMBL2021477 | — | Kd | = | 26.3 | nM | 7.58 |
| CHEMBL2021478 | — | Kd | = | 26.92 | nM | 7.57 |
| CHEMBL9967 | PIRENZEPINE | Kd | = | 131.83 | nM | 6.88 |
| CHEMBL265256 | TRIPITRAMINE | Kd | = | 281.84 | nM | 6.55 |
| CHEMBL478226 | — | Kd | = | 338.84 | nM | 6.47 |
| CHEMBL478227 | — | Kd | = | 977.24 | nM | 6.01 |