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Compound Detail

CHEMBL4760331

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O=C(NO)C1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1S(=O)(=O)c1ccc(-c2ccsc2)cc1

Basic Information

ChEMBL ID CHEMBL4760331
Phase Preclinical
Structure Type MOL
InChI Key CKFYTKAGHGFUPN-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

547.7
MW (Da)
4.10
ALogP
6
HBA
2
HBD
107.0
PSA (Ų)
0.28
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25N3O5S2
MW 547.66
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.61

Activity Summary

EC50 1 meas. best 5.22
Ki 1 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 5.22 5.22 6000.0 1
Falcilysin
CHEMBL4295876
Ki 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum EC50 = 6000.0 nM 5.22 Parasiticidal activity against Plasmodium falciparum 3D7 33227414
Falcilysin Ki = 11000.0 nM 4.96 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