Compound Detail
CHEMBL566534
ARTEMETHER 💊 Approved Drug
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💊 Approved Drug
CO[C@H]1O[C@@H]2O[C@@]3(C)CC[C@H]4[C@H](C)CC[C@@H]([C@H]1C)[C@@]24OO3
Basic Information
| ChEMBL ID | CHEMBL566534 |
| Name | ARTEMETHER |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | SXYIRMFQILZOAM-HVNFFKDJSA-N |
| Therapeutic | ✓ Yes |
| Active Moiety | CHEMBL307261 |
16
Targets
59
Activities
2
Assay Types
17
PK Parameters
20
Publications
17
Known Names
7
Indications
1
Mechanisms
Molecular Properties
298.4
MW (Da)
2.84
ALogP
5
HBA
0
HBD
46.1
PSA (Ų)
0.70
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2009 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
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 Neoplasms
ATC Classification
P01BE02
artemether
Level 1: ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
Level 2: ANTIPROTOZOALS
Activity Summary
IC50 58 meas. best 8.9
EC50 1 meas. best 5.28
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Plasmodium falciparum CHEMBL364 | IC50 | 8.9 | 8.3744 | 1.3 | 39 |
| Plasmodium berghei CHEMBL612653 | IC50 | 8.52 | 8.08 | 3.0 | 2 |
| Toxoplasma gondii CHEMBL612888 | IC50 | 6.51 | 6.51 | 310.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.46 | 6.46 | 351.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 5.75 | 5.1433 | 1780.0 | 3 |
| T-cell CHEMBL614309 | IC50 | 5.42 | 5.42 | 3820.0 | 1 |
| Cytomegalovirus CHEMBL613134 | EC50 | 5.28 | 5.28 | 5300.0 | 1 |
| Prostaglandin E synthase 2 CHEMBL4411 | IC50 | 5.14 | 5.14 | 7200.0 | 1 |
| SK-MEL-2 CHEMBL614917 | IC50 | 5.14 | 5.14 | 7240.0 | 1 |
| SK-OV-3 CHEMBL614925 | IC50 | 5.09 | 5.09 | 8030.0 | 1 |
| A549 CHEMBL392 | IC50 | 5.07 | 5.07 | 8540.0 | 1 |
| HCT-116 CHEMBL394 | IC50 | 5.07 | 5.07 | 8600.0 | 1 |
| XF498 CHEMBL613533 | IC50 | 5.04 | 5.04 | 9100.0 | 1 |
| HCT-15 CHEMBL612263 | IC50 | 5.01 | 5.01 | 9660.0 | 1 |
| Leishmania major CHEMBL612879 | IC50 | 4.65 | 4.65 | 22540.0 | 1 |
| Leishmania donovani CHEMBL367 | IC50 | 4.37 | 4.205 | 42290.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 168.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 382.0 | ng.hr.mL-1 | Homo sapiens |
| CL | 114.0 | mL.min-1.kg-1 | Mus musculus |
| Cmax | 113.95 | nM | Homo sapiens |
| Cmax | 398.82 | nM | Homo sapiens |
| F | 1.4 | % | Rattus norvegicus |
| F | 1.4 | % | Mus musculus |
| F | 1.4 | % | Rattus norvegicus |
| F | 1.4 | % | Rattus norvegicus |
| T1/2 | 2.0 | hr | - |
| T1/2 | 52.2 | - | Rattus norvegicus |
| T1/2 | 0.8667 | hr | Mus musculus |
| T1/2 | 3.9 | hr | Homo sapiens |
| T1/2 | 1.9 | hr | Homo sapiens |
| T1/2 | 1.0 | hr | Homo sapiens |
| T1/2 | 11.0 | hr | - |
| Vd | 8.0 | L.kg-1 | Mus musculus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine