Compound Detail
CHEMBL58323
LACOSAMIDE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL58323 |
| Name | LACOSAMIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | VPPJLAIAVCUEMN-GFCCVEGCSA-N |
| Therapeutic | ✓ Yes |
18
Targets
23
Activities
2
Assay Types
0
PK Parameters
20
Publications
17
Known Names
20
Indications
1
Mechanisms
Molecular Properties
250.3
MW (Da)
0.45
ALogP
3
HBA
2
HBD
67.4
PSA (Ų)
0.77
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2008 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Sodium channel alpha subunit blocker | BLOCKER | Sodium channel alpha subunit | ✓ | ✓ |
Indications
Epilepsies, Partial Epilepsy Epilepsy Seizures Anxiety Dementia Depressive Disorder Diabetic Neuropathies Erythromelalgia Migraine Disorders Schizophrenia Sciatica Status Epilepticus Alcoholism Brain Neoplasms Fibromyalgia Neuralgia Neuralgia, Postherpetic Osteoarthritis Paraganglioma
ATC Classification
N03AX18
lacosamide
Level 1: NERVOUS SYSTEM
Level 2: ANTIEPILEPTICS
Activity Summary
Ki 13 meas. best 6.48
IC50 10 meas. best 6.74
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Sodium channel protein type 9 subunit alpha CHEMBL4296 | IC50 | 6.74 | 6.74 | 182.0 | 1 |
| Carbonic anhydrase 2 CHEMBL205 | Ki | 6.48 | 6.48 | 331.0 | 1 |
| Carbonic anhydrase 5B, mitochondrial CHEMBL3969 | Ki | 6.47 | 6.47 | 341.0 | 1 |
| Carbonic anhydrase 9 CHEMBL3594 | Ki | 6.45 | 6.45 | 353.0 | 1 |
| Carbonic anhydrase 1 CHEMBL261 | Ki | 6.44 | 6.44 | 362.0 | 1 |
| Carbonic anhydrase 3 CHEMBL2885 | Ki | 6.43 | 6.43 | 374.0 | 1 |
| Carbonic anhydrase 6 CHEMBL3025 | Ki | 6.38 | 6.38 | 412.0 | 1 |
| Sodium channel protein type 3 subunit alpha CHEMBL4966 | IC50 | 6.38 | 6.38 | 415.0 | 2 |
| Carbonic anhydrase 15 CHEMBL5973 | Ki | 6.34 | 6.34 | 461.0 | 1 |
| Carbonic anhydrase 14 CHEMBL3510 | Ki | 6.33 | 6.33 | 473.0 | 1 |
| Carbonic anhydrase 4 CHEMBL3729 | Ki | 6.28 | 6.28 | 525.0 | 1 |
| Carbonic anhydrase 13 CHEMBL3912 | Ki | 5.92 | 5.92 | 1210.0 | 1 |
| Carbonic anhydrase 12 CHEMBL3242 | Ki | 5.43 | 5.43 | 3713.0 | 1 |
| Carbonic anhydrase 7 CHEMBL2326 | Ki | 5.35 | 5.35 | 4446.0 | 1 |
| Carbonic anhydrase 5A, mitochondrial CHEMBL4789 | Ki | 5.34 | 5.34 | 4565.0 | 1 |
| Sodium channel protein type 10 subunit alpha CHEMBL4017 | IC50 | 4.8 | 4.8 | 16000.0 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C CHEMBL1940 | IC50 | 4.3 | 4.3 | 50118.7 | 1 |
| Unchecked CHEMBL612545 | IC50 | 4.07 | 4.07 | 85000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine