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Compound Detail

CHEMBL4741390

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CNC(=O)C1CN(S(=O)(=O)c2ccc(-c3ccccc3)cc2)CCN1S(=O)(=O)c1cccc(CCc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL4741390
Phase Preclinical
Structure Type MOL
InChI Key GSNCZJCSSFQKLX-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

603.8
MW (Da)
3.95
ALogP
5
HBA
1
HBD
103.9
PSA (Ų)
0.31
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H33N3O5S2
MW 603.77
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.16

Activity Summary

EC50 1 meas. best 5.68
Ki 1 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 5.68 5.68 2100.0 1
Falcilysin
CHEMBL4295876
Ki 5.6 5.6 2500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum EC50 = 2100.0 nM 5.68 Parasiticidal activity against Plasmodium falciparum 3D7 33227414
Falcilysin Ki = 2500.0 nM 5.6 Inhibition of Plasmodium falciparum FLN 33227414

Literature References

PubMed DOI Target Context # Activities
33227414 10.1016/j.bmcl.2020.127683 Falcilysin 1
33227414 10.1016/j.bmcl.2020.127683 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine