Assay Detail
Binding
CHEMBL929996
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Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells by wash-resistant binding method
20
Total Activities
20
Compounds Tested
2
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 | 11 | 4.86 | 5.67 |
| Activity | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL291351 | — | — | 1 | 5.67 |
| CHEMBL406802 | — | — | 1 | 5.40 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 5.31 |
| CHEMBL327754 | — | — | 1 | 5.07 |
| CHEMBL99768 | — | — | 1 | 5.04 |
| CHEMBL270031 | — | — | 1 | 4.83 |
| CHEMBL408822 | — | — | 1 | 4.54 |
| CHEMBL255791 | — | — | 1 | 4.35 |
| CHEMBL272468 | — | — | 1 | 4.28 |
| CHEMBL101054 | — | — | 1 | 4.11 |
| CHEMBL405125 | — | — | 1 | - |
| CHEMBL272359 | — | — | 1 | - |
| CHEMBL406570 | — | — | 1 | - |
| CHEMBL255793 | — | — | 1 | - |
| CHEMBL403829 | — | — | 1 | - |
| CHEMBL401694 | — | — | 1 | - |
| CHEMBL257683 | — | — | 1 | - |
| CHEMBL271774 | — | — | 1 | - |
| CHEMBL99476 | — | — | 1 | - |
| CHEMBL303922 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL291351 | — | IC50 | = | 2137.96 | nM | 5.67 |
| CHEMBL406802 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL327754 | — | IC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL99768 | — | IC50 | = | 9120.11 | nM | 5.04 |
| CHEMBL270031 | — | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL408822 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL255791 | — | IC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL272468 | — | IC50 | = | 52480.75 | nM | 4.28 |
| CHEMBL101054 | — | IC50 | = | 77624.71 | nM | 4.11 |
| CHEMBL405125 | — | Activity | - | — | - | |
| CHEMBL272359 | — | Activity | - | — | - | |
| CHEMBL406570 | — | IC50 | = | 109647.82 | nM | - |
| CHEMBL255793 | — | Activity | - | — | - | |
| CHEMBL403829 | — | Activity | - | — | - | |
| CHEMBL401694 | — | Activity | - | — | - | |
| CHEMBL257683 | — | Activity | - | — | - | |
| CHEMBL271774 | — | Activity | - | — | - | |
| CHEMBL99476 | — | Activity | - | — | - | |
| CHEMBL303922 | — | Activity | - | — | - |