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Compound Detail

CHEMBL205056

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COC(=O)c1ccsc1NC(=O)CN1CCN(S(=O)(=O)c2ccc(Cl)cc2)CC1

Basic Information

ChEMBL ID CHEMBL205056
Phase Preclinical
Structure Type MOL
InChI Key SXCQDTVDTJGKTQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

458.0
MW (Da)
2.13
ALogP
7
HBA
1
HBD
96.0
PSA (Ų)
0.67
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 C18H20ClN3O5S2
MW 457.96
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -2.49

Activity Summary

IC50 2 meas. best 4.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Falcipain 2
CHEMBL5800
IC50 4.84 4.84 14300.0 1
Cysteine protease falcipain-3
CHEMBL4510
IC50 4.31 4.31 49200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Falcipain 2 IC50 = 14300.0 nM 4.84 Inhibition of falcipain2 16509575
Cysteine protease falcipain-3 IC50 = 49200.0 nM 4.31 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