Compound Detail
CHEMBL1200749
LEVOBUPIVACAINE HYDROCHLORIDE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1200749 |
| Name | LEVOBUPIVACAINE HYDROCHLORIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | SIEYLFHKZGLBNX-NTISSMGPSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL1201193 |
| Active Moiety | CHEMBL1201193 |
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
1
Publications
5
Known Names
2
Indications
1
Mechanisms
Molecular Properties
288.4
MW (Da)
3.90
ALogP
2
HBA
1
HBD
32.3
PSA (Ų)
0.89
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1999 |
| Availability | Discontinued |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Sodium channel protein type IV alpha subunit blocker | BLOCKER | Sodium channel protein type 4 subunit alpha | ✓ | ✓ |
Indications
Pain Pregnancy
Activity Summary
IC50 6 meas. best 4.89
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 4.89 | 4.62 | 13000.0 | 3 |
| Unchecked CHEMBL612545 | IC50 | 4.57 | 4.57 | 27170.6 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 13000.0 | nM | 4.89 | Inhibition of wild-type human ERG channel expressed in HEK293 cells assessed as ... | 21624711 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 13000.0 | nM | 4.89 | Inhibition of wild-type human ERG channel expressed in CHO cells by whole-cell p... | 21624711 |
| Unchecked | IC50 | = | 27170.63 | nM | 4.57 | PubChem BioAssay. insulin secretion from INS-1E cells in the presence of 5 mM gl... | - |
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 83000.0 | nM | 4.08 | Inhibition of human ERG Y652A mutant channel expressed in CHO cells by whole-cel... | 21624711 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 21624711 | 10.1016/j.ejmech.2011.05.015 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 5 |
Data from ChEMBL 36 via Core Engine