Assay Detail
Functional
CHEMBL2215475
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Antagonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as inhibition of carbachol induced calcium response by fluorescence assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 2 | - | - |
| IC50 | 2 | 5.98 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206333 | — | — | 2 | 6.52 |
| CHEMBL2206335 | — | — | 2 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206333 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2206335 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL2206335 | — | Inhibition | - | % | - | |
| CHEMBL2206333 | — | Inhibition | - | % | - |