Compound Detail
CHEMBL1200803
SOLIFENACIN SUCCINATE 💊 Approved Drug
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💊 Approved Drug
O=C(O)CCC(=O)O.O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
Basic Information
| ChEMBL ID | CHEMBL1200803 |
| Name | SOLIFENACIN SUCCINATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RXZMMZZRUPYENV-VROPFNGYSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL1734 |
| Active Moiety | CHEMBL1734 |
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
10
Publications
7
Known Names
3
Indications
2
Mechanisms
Molecular Properties
362.5
MW (Da)
3.86
ALogP
3
HBA
0
HBD
32.8
PSA (Ų)
0.81
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2004 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Muscarinic acetylcholine receptor M3 antagonist | ANTAGONIST | Muscarinic acetylcholine receptor M3 | ✓ | ✓ |
| Muscarinic acetylcholine receptor M2 antagonist | ANTAGONIST | Muscarinic acetylcholine receptor M2 | ✓ | ✓ |
Indications
Urinary Bladder, Overactive Urinary Incontinence, Urge Prostatic Hyperplasia
Activity Summary
IC50 3 meas. best 7.2
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 7.2 | 7.2 | 63.5 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | IC50 | 6.88 | 6.88 | 130.8 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | IC50 | 6.24 | 6.24 | 573.7 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | IC50 | = | 63.5 | nM | 7.2 | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 ce... | 21524581 |
| Muscarinic acetylcholine receptor M3 | IC50 | = | 130.8 | nM | 6.88 | Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 ce... | 21524581 |
| Muscarinic acetylcholine receptor M2 | IC50 | = | 573.7 | nM | 6.24 | Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 ce... | 21524581 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.5281/zenodo.13943903 | ADMET | 89 |
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 21524581 | 10.1016/j.bmcl.2011.03.096 | Muscarinic acetylcholine receptor M3 | 1 |
| 21524581 | 10.1016/j.bmcl.2011.03.096 | Muscarinic acetylcholine receptor M2 | 1 |
| 21524581 | 10.1016/j.bmcl.2011.03.096 | Muscarinic acetylcholine receptor M1 | 1 |
| 21524581 | 10.1016/j.bmcl.2011.03.096 | Muscarinic acetylcholine receptors; M2 & M3 | 1 |
| 21524581 | 10.1016/j.bmcl.2011.03.096 | Muscarinic acetylcholine receptor M1 and M3 | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine