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Compound Detail

CHEMBL3218779

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COc1ccc(C(=O)Nc2ccc3nc(SCC(=O)c4ccccc4)sc3c2)cc1

Basic Information

ChEMBL ID CHEMBL3218779
Phase Preclinical
Structure Type MOL
InChI Key PNGZHWIJXJLVRQ-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
5.53
ALogP
6
HBA
1
HBD
68.3
PSA (Ų)
0.31
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18N2O3S2
MW 434.54
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.96

Activity Summary

IC50 4 meas. best 5.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cathepsin K
CHEMBL268
IC50 5.21 5.21 6120.0 1
Unchecked
CHEMBL612545
IC50 4.99 4.99 10300.0 1
Cathepsin B
CHEMBL4072
IC50 4.75 4.75 17660.0 1
Procathepsin L
CHEMBL3837
IC50 4.5 4.5 31630.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cathepsin K IC50 = 6120.0 nM 5.21 Inhibition of human cathepsin K -
Unchecked IC50 = 10300.0 nM 4.99 Inhibition of Plasmodium falciparum recombinant falcipain 2 -
Cathepsin B IC50 = 17660.0 nM 4.75 Inhibition of human cathepsin B -
Procathepsin L IC50 = 31630.0 nM 4.5 Inhibition of human cathepsin L1 -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C1MD00129A Unchecked 2
- 10.1039/C1MD00129A Plasmodium falciparum 1
- 10.1039/C1MD00129A Cathepsin K 1
- 10.1039/C1MD00129A Procathepsin L 1
- 10.1039/C1MD00129A Cathepsin B 1

Data from ChEMBL 36 via Core Engine