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Compound Detail

CHEMBL255086

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COc1ccc(CNc2nc(C#N)nc3c2ncn3Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL255086
Phase Preclinical
Structure Type MOL
InChI Key OYSZBLDJZXWWEI-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

370.4
MW (Da)
3.37
ALogP
7
HBA
1
HBD
88.7
PSA (Ų)
0.56
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 C21H18N6O
MW 370.42
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 5.35
EC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
EC50 6.0 6.0 1000.0 1
Cathepsin B-like cysteine protease
CHEMBL5832
IC50 5.35 5.35 4500.0 1
Procathepsin L
CHEMBL3837
IC50 5.09 5.09 8050.0 1

Activity Data Samples

Top measurements by pChEMBL value

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