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Compound Detail

CHEMBL4580614

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CCCCCc1ccc(C(=O)N(Cc2ccc(-c3ccc(OC)cc3)cc2)C2CCN(CCC(C)C)CC2)cc1

Basic Information

ChEMBL ID CHEMBL4580614
Phase Preclinical
Structure Type MOL
InChI Key BGRDACPMBHDXJD-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

540.8
MW (Da)
8.25
ALogP
3
HBA
0
HBD
32.8
PSA (Ų)
0.20
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H48N2O2
MW 540.79
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.94

Activity Summary

IC50 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmepsin II
CHEMBL4414
IC50 8.1 8.1 8.0 1
Cathepsin D
CHEMBL2581
IC50 5.36 5.36 4400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmepsin II IC50 = 8.0 nM 8.1 Inhibition of recombinant Plasmodium falciparum Plasmepsin 2 by FRET assay 31913032
Cathepsin D IC50 = 4400.0 nM 5.36 Inhibition of human cathepsin D 31913032

Literature References

PubMed DOI Target Context # Activities
31913032 10.1021/acs.jmedchem.9b01622 Cathepsin D 1
31913032 10.1021/acs.jmedchem.9b01622 Plasmepsin II 1

Data from ChEMBL 36 via Core Engine