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Compound Detail

CHEMBL452345

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COc1cccc(OCC(=O)N[C@@H](Cc2ccccc2)[C@H](O)C(=O)N2CSC(C)(C)[C@H]2C(=O)N[C@H]2c3ccccc3C[C@H]2O)c1

Basic Information

ChEMBL ID CHEMBL452345
Phase Preclinical
Structure Type MOL
InChI Key JUVIZUPSXSIJMO-VFCPCCRCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

633.8
MW (Da)
2.62
ALogP
8
HBA
4
HBD
137.4
PSA (Ų)
0.25
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H39N3O7S
MW 633.77
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness 0.13

Activity Summary

Ki 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmepsin II
CHEMBL4414
Ki 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmepsin II Ki = 4.0 nM 8.4 Inhibition of Plasmodium falciparum plasmepsin-2 18952439

Literature References

PubMed DOI Target Context # Activities
18952439 10.1016/j.bmc.2008.10.011 Plasmepsin II 1
18952439 10.1016/j.bmc.2008.10.011 Protease 1
18952439 10.1016/j.bmc.2008.10.011 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine