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Compound Detail

CHEMBL469416

ALPHA-ARTEETHER
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CCO[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 CHEMBL469416
Name ALPHA-ARTEETHER
Phase Preclinical
Structure Type MOL
InChI Key NLYNIRQVMRLPIQ-VBGZEHGNSA-N
1
Targets
4
Activities
1
Assay Types
30
PK Parameters
10
Publications
0
Known Names

Molecular Properties

312.4
MW (Da)
3.23
ALogP
5
HBA
0
HBD
46.1
PSA (Ų)
0.73
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C17H28O5
MW 312.41
Aromatic Rings 0
Heavy Atoms 22
NP-Likeness 3.54

Activity Summary

IC50 4 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 8.68 8.5425 2.1 4

Pharmacokinetic Data

Parameter Value Units Species
AUC 1303.1 ng.hr.mL-1 Homo sapiens
AUC 754.4 ng.hr.mL-1 Macaca mulatta
AUC 641.8 ng.hr.mL-1 Macaca mulatta
AUC 6.6 ng.hr.mL-1 Macaca mulatta
AUC 73.8 ng.hr.mL-1 Rattus norvegicus
AUC 131.7 ng.hr.mL-1 Rattus norvegicus
AUC 111.5 ng.hr.mL-1 Rattus norvegicus
AUC 50.9 ng.hr.mL-1 Rattus norvegicus
AUC 601.1 ng.hr.mL-1 Rattus norvegicus
AUC 1247.1 ng.hr.mL-1 Rattus norvegicus
AUC 1058.5 ng.hr.mL-1 Rattus norvegicus
CL 10.0 mL.min-1.kg-1 Homo sapiens
CL 26.67 mL.min-1.kg-1 Macaca mulatta
CL 61.67 mL.min-1.kg-1 Macaca mulatta
CL 30771.67 mL.min-1.kg-1 Macaca mulatta
CL 600.0 mL.min-1.kg-1 Rattus norvegicus
CL 75.0 mL.min-1.kg-1 Rattus norvegicus
CL 1331.67 mL.min-1.kg-1 Rattus norvegicus
CL 1708.33 mL.min-1.kg-1 Rattus norvegicus
CL 246.67 mL.min-1.kg-1 Rattus norvegicus
CL 68.33 mL.min-1.kg-1 Rattus norvegicus
CL 40.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 194.3 nM Homo sapiens
Cmax 309.53 nM Macaca mulatta
Cmax 12.48 nM Macaca mulatta
Cmax 106.91 nM Rattus norvegicus
Cmax 329.05 nM Rattus norvegicus
Cmax 120.35 nM Rattus norvegicus
Cmax 298.65 nM Rattus norvegicus
Cmax 587.69 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1007/s00044-004-0053-3 Rattus norvegicus 54
3279208 10.1021/jm00398a026 Plasmodium berghei 26
- 10.1007/s00044-004-0053-3 Rhesus monkey 22
- 10.1007/s00044-004-0053-3 Homo sapiens 8
3279208 10.1021/jm00398a026 Plasmodium falciparum 4
17125275 10.1021/jm060826x Plasmodium yoelii nigeriensis 2
17125275 10.1021/jm060826x Trypanosoma brucei rhodesiense 2
16124777 10.1021/np050074u Candida albicans 2
16124777 10.1021/np050074u Cryptococcus neoformans 2
17125275 10.1021/jm060826x No relevant target 1

Data from ChEMBL 36 via Core Engine