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Compound Detail

CHEMBL162898

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CC(C)[C@H](NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN[C@@H](Cc1cccc(OS(=O)(=O)C(F)(F)F)c1)C(N)=O

Basic Information

ChEMBL ID CHEMBL162898
Phase Preclinical
Structure Type MOL
InChI Key SWSGGJCLZRKYQH-FWEHEUNISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

679.7
MW (Da)
1.84
ALogP
9
HBA
5
HBD
189.8
PSA (Ų)
0.11
QED
1
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H36F3N5O7S
MW 679.72
Aromatic Rings 3
Heavy Atoms 47
NP-Likeness -0.34

Activity Summary

Ki 2 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmepsin I
CHEMBL4687
Ki 6.33 6.33 469.0 1
Cathepsin D
CHEMBL2581
Ki 5.77 5.77 1700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmepsin I Ki = 469.0 nM 6.33 Binding affinity for Plasmodium falciparum plasmepsin-1. 12593654
Cathepsin D Ki = 1700.0 nM 5.77 In vitro binding affinity for human cathepsin D. 12593654

Literature References

PubMed DOI Target Context # Activities
12593654 10.1021/jm020951i Plasmepsin I 1
12593654 10.1021/jm020951i Plasmepsin II 1
12593654 10.1021/jm020951i Cathepsin D 1

Data from ChEMBL 36 via Core Engine