Assay Detail
Binding
CHEMBL929995
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Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in continuous presence of radioligand
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.42 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL101054 | — | — | 1 | 7.55 |
| CHEMBL327754 | — | — | 1 | 7.48 |
| CHEMBL291351 | — | — | 1 | 7.43 |
| CHEMBL303922 | — | — | 1 | 7.28 |
| CHEMBL405125 | — | — | 1 | 7.23 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.09 |
| CHEMBL99476 | — | — | 1 | 6.85 |
| CHEMBL99768 | — | — | 1 | 6.84 |
| CHEMBL270031 | — | — | 1 | 6.79 |
| CHEMBL408822 | — | — | 1 | 6.56 |
| CHEMBL403829 | — | — | 1 | 6.51 |
| CHEMBL271774 | — | — | 1 | 6.21 |
| CHEMBL406802 | — | — | 1 | 6.19 |
| CHEMBL272468 | — | — | 1 | 6.06 |
| CHEMBL406570 | — | — | 1 | 6.00 |
| CHEMBL257683 | — | — | 1 | 5.97 |
| CHEMBL255791 | — | — | 1 | 5.72 |
| CHEMBL401694 | — | — | 1 | 5.42 |
| CHEMBL272359 | — | — | 1 | 5.15 |
| CHEMBL255793 | — | — | 1 | 4.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL101054 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL327754 | — | IC50 | = | 33.11 | nM | 7.48 |
| CHEMBL291351 | — | IC50 | = | 37.15 | nM | 7.43 |
| CHEMBL303922 | — | IC50 | = | 52.48 | nM | 7.28 |
| CHEMBL405125 | — | IC50 | = | 58.88 | nM | 7.23 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 81.28 | nM | 7.09 |
| CHEMBL99476 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL99768 | — | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL270031 | — | IC50 | = | 162.18 | nM | 6.79 |
| CHEMBL408822 | — | IC50 | = | 275.42 | nM | 6.56 |
| CHEMBL403829 | — | IC50 | = | 309.03 | nM | 6.51 |
| CHEMBL271774 | — | IC50 | = | 616.6 | nM | 6.21 |
| CHEMBL406802 | — | IC50 | = | 645.65 | nM | 6.19 |
| CHEMBL272468 | — | IC50 | = | 870.96 | nM | 6.06 |
| CHEMBL406570 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL257683 | — | IC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL255791 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL401694 | — | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL272359 | — | IC50 | = | 7079.46 | nM | 5.15 |
| CHEMBL255793 | — | IC50 | = | 77624.71 | nM | 4.11 |