Compound Detail
CHEMBL2111051
TALSACLIDINE 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL2111051 |
| Name | TALSACLIDINE |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | XVFJONKUSLSKSW-JTQLQIEISA-N |
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
2
Known Names
1
Indications
3
Mechanisms
Molecular Properties
165.2
MW (Da)
0.73
ALogP
2
HBA
0
HBD
12.5
PSA (Ų)
0.56
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Muscarinic acetylcholine receptor M3 partial agonist | PARTIAL AGONIST | Muscarinic acetylcholine receptor M3 | ✓ | ✓ |
| Muscarinic acetylcholine receptor M2 partial agonist | PARTIAL AGONIST | Muscarinic acetylcholine receptor M2 | ✓ | ✓ |
| Muscarinic acetylcholine receptor M1 agonist | AGONIST | Muscarinic acetylcholine receptor M1 | ✓ | ✓ |
Indications
Alzheimer Disease
Activity Summary
EC50 5 meas. best 6.38
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | EC50 | 6.38 | 6.38 | 422.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | EC50 | 6.09 | 6.09 | 820.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | EC50 | 6.07 | 6.07 | 844.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | EC50 | 6.07 | 6.07 | 849.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | EC50 | 5.57 | 5.57 | 2696.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M5 | EC50 | = | 422.0 | nM | 6.38 | Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30... | 26299349 |
| Muscarinic acetylcholine receptor M1 | EC50 | = | 820.0 | nM | 6.09 | Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30... | 26299349 |
| Muscarinic acetylcholine receptor M2 | EC50 | = | 849.0 | nM | 6.07 | Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30... | 26299349 |
| Muscarinic acetylcholine receptor M4 | EC50 | = | 844.0 | nM | 6.07 | Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30... | 26299349 |
| Muscarinic acetylcholine receptor M3 | EC50 | = | 2696.0 | nM | 5.57 | Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30... | 26299349 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 26299349 | 10.1016/j.bmcl.2015.08.011 | Muscarinic acetylcholine receptor M1 | 2 |
| 26299349 | 10.1016/j.bmcl.2015.08.011 | Muscarinic acetylcholine receptor M2 | 2 |
| 26299349 | 10.1016/j.bmcl.2015.08.011 | Muscarinic acetylcholine receptor M3 | 2 |
| 26299349 | 10.1016/j.bmcl.2015.08.011 | Muscarinic acetylcholine receptor M4 | 2 |
| 26299349 | 10.1016/j.bmcl.2015.08.011 | Muscarinic acetylcholine receptor M5 | 2 |
Data from ChEMBL 36 via Core Engine