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Compound Detail

CHEMBL591861

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COc1ccc(C2CC3=NC(C)=C(C(=O)OC(C)C)C(c4ccccc4Cl)C3=C(O)C2)cc1OC

Basic Information

ChEMBL ID CHEMBL591861
Phase Preclinical
Structure Type MOL
InChI Key PWLSMXYWLHWBDN-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

496.0
MW (Da)
6.51
ALogP
6
HBA
1
HBD
77.3
PSA (Ų)
0.46
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30ClNO5
MW 496.00
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.58

Activity Summary

EC50 2 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 8.39 8.3 4.1 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485428 10.1038/nature09099 Plasmodium falciparum 9
18579783 10.1073/pnas.0802982105 Plasmodium falciparum 2
18579783 10.1073/pnas.0802982105 Unchecked 1
18579783 10.1073/pnas.0802982105 Huh-7 1
20485428 10.1038/nature09099 Toxoplasma gondii 1
20485428 10.1038/nature09099 Trypanosoma brucei 1
20485428 10.1038/nature09099 HepG2 1
20485428 10.1038/nature09099 HEK293 1
20485428 10.1038/nature09099 Leishmania major 1
20485428 10.1038/nature09099 BJ 1
20485428 10.1038/nature09099 Raji 1
22096101 10.1126/science.1211936 Plasmodium yoelii 1

Data from ChEMBL 36 via Core Engine