Assay Detail
Functional
CHEMBL748279
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | A9L |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 7.21 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98255 | — | — | 1 | 9.30 |
| CHEMBL316625 | — | — | 1 | 9.00 |
| CHEMBL327269 | — | — | 1 | 9.00 |
| CHEMBL99521 | — | — | 1 | 7.80 |
| CHEMBL319109 | — | — | 1 | 7.55 |
| CHEMBL100163 | — | — | 1 | 7.17 |
| CHEMBL60419 | — | — | 1 | 7.15 |
| CHEMBL291351 | — | — | 1 | 6.96 |
| CHEMBL1169506 | — | — | 1 | 6.80 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.42 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 5.25 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 5.06 |
| CHEMBL81878 | — | — | 1 | - |
| CHEMBL99884 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98255 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL316625 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL327269 | — | EC50 | = | 0.99 | nM | 9.00 |
| CHEMBL99521 | — | EC50 | = | 15.7 | nM | 7.80 |
| CHEMBL319109 | — | EC50 | = | 28.3 | nM | 7.55 |
| CHEMBL100163 | — | EC50 | = | 67.3 | nM | 7.17 |
| CHEMBL60419 | — | EC50 | = | 70.5 | nM | 7.15 |
| CHEMBL291351 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1169506 | — | EC50 | = | 159.0 | nM | 6.80 |
| CHEMBL14 | CARBACHOL | EC50 | = | 3811.0 | nM | 5.42 |
| CHEMBL7303 | ARECOLINE | EC50 | = | 5603.0 | nM | 5.25 |
| CHEMBL550 | PILOCARPINE | EC50 | = | 8792.0 | nM | 5.06 |
| CHEMBL81878 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL99884 | — | EC50 | > | 100.0 | nM | - |