Assay Detail
Functional
CHEMBL880146
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was tested for its potency at M-2 receptor by inhibiting forskolin induced c-AMP formation in CHO-M2 cells human M2 receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO-M2 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.17 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60374 | — | — | 1 | 7.10 |
| CHEMBL418491 | — | — | 1 | 7.08 |
| CHEMBL291351 | — | — | 1 | 6.62 |
| CHEMBL60479 | — | — | 1 | 6.28 |
| CHEMBL303360 | — | — | 1 | 6.17 |
| CHEMBL304247 | — | — | 1 | 6.17 |
| CHEMBL60331 | — | — | 1 | 6.12 |
| CHEMBL294082 | — | — | 1 | 6.10 |
| CHEMBL417560 | — | — | 1 | 6.07 |
| CHEMBL293982 | — | — | 1 | 6.04 |
| CHEMBL60101 | — | — | 1 | 5.92 |
| CHEMBL60777 | — | — | 1 | 5.83 |
| CHEMBL64029 | — | — | 1 | 5.78 |
| CHEMBL60833 | — | — | 1 | 5.64 |
| CHEMBL291872 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60374 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL418491 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL291351 | — | EC50 | = | 241.0 | nM | 6.62 |
| CHEMBL60479 | — | EC50 | = | 528.0 | nM | 6.28 |
| CHEMBL303360 | — | EC50 | = | 673.0 | nM | 6.17 |
| CHEMBL304247 | — | EC50 | = | 683.0 | nM | 6.17 |
| CHEMBL60331 | — | EC50 | = | 763.0 | nM | 6.12 |
| CHEMBL294082 | — | EC50 | = | 791.0 | nM | 6.10 |
| CHEMBL417560 | — | EC50 | = | 853.0 | nM | 6.07 |
| CHEMBL293982 | — | EC50 | = | 904.0 | nM | 6.04 |
| CHEMBL60101 | — | EC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL60777 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL64029 | — | EC50 | = | 1655.0 | nM | 5.78 |
| CHEMBL60833 | — | EC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL291872 | — | EC50 | = | 2690.0 | nM | 5.57 |