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Compound Detail

CHEMBL487275

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COC(=O)/C=C/[C@H](CCc1ccccc1)n1cccc(NC(=O)OCc2ccccc2)c1=O

Basic Information

ChEMBL ID CHEMBL487275
Phase Preclinical
Structure Type MOL
InChI Key ZUABTEFINXPYNQ-QWYDYZLZSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
4.50
ALogP
6
HBA
1
HBD
86.6
PSA (Ų)
0.39
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26N2O5
MW 446.50
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.29

Activity Summary

IC50 3 meas. best 4.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Falcipain 2
CHEMBL5800
IC50 4.72 4.72 19000.0 1
Plasmodium falciparum
CHEMBL364
IC50 4.55 4.5 27900.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18554905 10.1016/j.bmcl.2008.05.068 Plasmodium falciparum 2
18554905 10.1016/j.bmcl.2008.05.068 Cysteine protease falcipain-3 1
18554905 10.1016/j.bmcl.2008.05.068 Falcipain 2 1

Data from ChEMBL 36 via Core Engine