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Compound Detail

CHEMBL3236059

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COC(CNc1cc(C)c(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)c(C)c1)OC

Basic Information

ChEMBL ID CHEMBL3236059
Phase Preclinical
Structure Type MOL
InChI Key PKSJBPCALNNZRC-XEJIMHFWSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

734.9
MW (Da)
3.26
ALogP
10
HBA
5
HBD
158.7
PSA (Ų)
0.15
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H50N4O8S
MW 734.92
Aromatic Rings 3
Heavy Atoms 52
NP-Likeness 0.06

Activity Summary

EC50 1 meas. best 6.07
Ki 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmepsin II
CHEMBL4414
Ki 7.96 7.96 11.0 1
Plasmodium falciparum
CHEMBL364
EC50 6.07 6.07 850.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24631188 10.1016/j.bmcl.2014.02.051 Plasmodium falciparum 2
24631188 10.1016/j.bmcl.2014.02.051 Plasmepsin II 1

Data from ChEMBL 36 via Core Engine