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Compound Detail

CHEMBL379228

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Cc1ccc(S(=O)(=O)NC(=O)NCC2CCN(S(=O)(=O)c3ccccc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL379228
Phase Preclinical
Structure Type MOL
InChI Key FMEDEMQOSFQPTG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

451.6
MW (Da)
2.08
ALogP
5
HBA
2
HBD
112.7
PSA (Ų)
0.70
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N3O5S2
MW 451.57
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.63

Activity Summary

IC50 2 meas. best 4.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Falcipain 2
CHEMBL5800
IC50 4.72 4.72 19000.0 1
Cysteine protease falcipain-3
CHEMBL4510
IC50 4.47 4.47 34000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Falcipain 2 IC50 = 19000.0 nM 4.72 Inhibition of falcipain2 16509575
Cysteine protease falcipain-3 IC50 = 34000.0 nM 4.47 Inhibition of falcipain3 16509575

Literature References

PubMed DOI Target Context # Activities
16509575 10.1021/jm0505765 Falcipain 2 1
16509575 10.1021/jm0505765 Cysteine protease falcipain-3 1

Data from ChEMBL 36 via Core Engine