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Compound Detail

CHEMBL402465

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Cc1ccc(/C(=N/NC(N)=S)c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL402465
Phase Preclinical
Structure Type MOL
InChI Key DZOZYORQEZEOCT-SAPNQHFASA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

269.4
MW (Da)
2.58
ALogP
2
HBA
2
HBD
50.4
PSA (Ų)
0.51
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N3S
MW 269.37
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -1.29

Activity Summary

IC50 3 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.3 6.3 500.0 1
Procathepsin L
CHEMBL3837
IC50 5.99 5.99 1020.0 1
Cathepsin B
CHEMBL4072
IC50 4.89 4.89 13000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 500.0 nM 6.3 Inhibition of Trypanosoma brucei rhodesain 18420405
Procathepsin L IC50 = 1020.0 nM 5.99 Inhibition of human cathepsin L 18420405
Cathepsin B IC50 = 13000.0 nM 4.89 Inhibition of human cathepsin B 18420405

Literature References

PubMed DOI Target Context # Activities
19447616 10.1016/j.bmcl.2009.04.142 Plasmodium falciparum 4
18420405 10.1016/j.bmcl.2008.03.083 Unchecked 2
18420405 10.1016/j.bmcl.2008.03.083 Trypanosoma brucei 1
18420405 10.1016/j.bmcl.2008.03.083 Procathepsin L 1
18420405 10.1016/j.bmcl.2008.03.083 Cathepsin B 1

Data from ChEMBL 36 via Core Engine