Compound Detail
CHEMBL4594214
ZICONOTIDE 💊 Approved Drug
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💊 Approved Drug
CSCC[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC3=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O
Basic Information
| ChEMBL ID | CHEMBL4594214 |
| Name | ZICONOTIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | BPKIMPVREBSLAJ-QTBYCLKRSA-N |
| Therapeutic | ✓ Yes |
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
4
Known Names
2
Indications
1
Mechanisms
Molecular Properties
2639.2
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2004 |
| Availability | Unknown |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Voltage-gated N-type calcium channel alpha-1B subunit blocker | BLOCKER | Voltage-dependent N-type calcium channel subunit alpha-1B | ✓ | ✓ |
Indications
Fever Pain
ATC Classification
N02BG08
ziconotide
Level 1: NERVOUS SYSTEM
Level 2: ANALGESICS
Activity Summary
IC50 2 meas. best 6.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Voltage-dependent N-type calcium channel subunit alpha-1B CHEMBL4478 | IC50 | 6.3 | 6.26 | 500.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Voltage-dependent N-type calcium channel subunit alpha-1B | IC50 | = | 500.0 | nM | 6.3 | In vitro antagonism of N-type calcium channels expressed in PC12 cells was deter... | 15537361 |
| Voltage-dependent N-type calcium channel subunit alpha-1B | IC50 | = | 600.0 | nM | 6.22 | In vitro antagonism of N-type calcium channels expressed in PC12 cells was deter... | 15537361 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 33538583 | 10.1021/acs.jmedchem.0c01726 | ADMET | 6 |
| 15537361 | 10.1021/jm049923l | Voltage-dependent N-type calcium channel subunit alpha-1B | 2 |
| 33538583 | 10.1021/acs.jmedchem.0c01726 | Rattus norvegicus | 2 |
| 38691890 | 10.1016/j.ejmech.2024.116456 | ADMET | 1 |
Data from ChEMBL 36 via Core Engine