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Compound Detail

CHEMBL400096

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CCCCn1cnc2c(NCc3ccc(C)cc3)nc(C#N)nc21

Basic Information

ChEMBL ID CHEMBL400096
Phase Preclinical
Structure Type MOL
InChI Key VZJXSBONGBQGBX-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

320.4
MW (Da)
3.42
ALogP
6
HBA
1
HBD
79.4
PSA (Ų)
0.75
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 C18H20N6
MW 320.40
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.34

Activity Summary

EC50 1 meas. best 6.26
IC50 1 meas. best 5.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
EC50 6.26 6.26 550.0 1
Procathepsin L
CHEMBL3837
IC50 5.23 5.23 5860.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei EC50 = 550.0 nM 6.26 Antitrypanosomal activity against Trypanosoma brucei 18173229
Procathepsin L IC50 = 5860.0 nM 5.23 Inhibition of human liver cathepsin L 18173229

Literature References

PubMed DOI Target Context # Activities
18173229 10.1021/jm070760l Cathepsin B-like cysteine protease 1
18173229 10.1021/jm070760l Trypanosoma brucei 1
18173229 10.1021/jm070760l Procathepsin L 1
18173229 10.1021/jm070760l Cathepsin B 1

Data from ChEMBL 36 via Core Engine