Compound Detail
CHEMBL38827
LUMEFANTRINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL38827 |
| Name | LUMEFANTRINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | DYLGFOYVTXJFJP-MYYYXRDXSA-N |
| Therapeutic | ✓ Yes |
3
Targets
75
Activities
2
Assay Types
19
PK Parameters
20
Publications
9
Known Names
6
Indications
1
Mechanisms
Molecular Properties
529.0
MW (Da)
9.15
ALogP
2
HBA
1
HBD
23.5
PSA (Ų)
0.22
QED
2
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2009 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Ferriprotoporphyrin IX inhibitor | INHIBITOR | Ferriprotoporphyrin IX | ✓ | ✓ |
Indications
Malaria Fever Malaria, Falciparum Malaria, Vivax Schistosomiasis haematobia HIV Infections
Activity Summary
IC50 72 meas. best 9.72
EC50 3 meas. best 9.35
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Plasmodium falciparum CHEMBL364 | IC50 | 9.72 | 7.95 | 0.2 | 63 |
| Plasmodium falciparum CHEMBL364 | EC50 | 9.35 | 7.25 | 0.5 | 3 |
| Plasmodium vivax CHEMBL613013 | IC50 | 7.84 | 7.63 | 14.6 | 5 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.42 | 5.755 | 377.0 | 4 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 210040.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 194740.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 472000.0 | ng.hr.mL-1 | Homo sapiens |
| CL | 6.11 | L/hr | Homo sapiens |
| CL | 1.82 | L/hr | Homo sapiens |
| Cmax | 12774.36 | nM | Homo sapiens |
| Cmax | 3922.87 | nM | Homo sapiens |
| Cmax | 4692.31 | nM | Homo sapiens |
| Cmax | 4588.34 | nM | Homo sapiens |
| Cmax | 593.63 | nM | Homo sapiens |
| Cmax | 941.49 | nM | Homo sapiens |
| Cmax | 818.6 | nM | Homo sapiens |
| Cmax | 92.64 | nM | Homo sapiens |
| Ka | 0.0588 | /hr | Homo sapiens |
| T1/2 | 32.7 | hr | Homo sapiens |
| T1/2 | 79.2 | hr | Homo sapiens |
| T1/2 | 72.0 | hr | Homo sapiens |
| Vz | 20.2 | l | Homo sapiens |
| Vz | 181.0 | l | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine