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Compound Detail

CHEMBL444759

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Cc1cc(NCc2cccnc2)cc(C)c1OCC(=O)N[C@@H](Cc1ccccc1)[C@H](O)C(=O)N1CSC(C)(C)[C@H]1C(=O)N[C@H]1c2ccccc2C[C@H]1O

Basic Information

ChEMBL ID CHEMBL444759
Phase Preclinical
Structure Type MOL
InChI Key HBTCIJNHNMLBFP-CTRNRRKFSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

737.9
MW (Da)
4.23
ALogP
9
HBA
5
HBD
153.1
PSA (Ų)
0.14
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H47N5O6S
MW 737.92
Aromatic Rings 4
Heavy Atoms 53
NP-Likeness -0.17

Activity Summary

EC50 1 meas. best 6.3
Ki 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmepsin II
CHEMBL4414
Ki 7.68 7.68 21.0 1
Plasmodium falciparum
CHEMBL364
EC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

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
18952439 10.1016/j.bmc.2008.10.011 L6 1

Data from ChEMBL 36 via Core Engine