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Compound Detail

CHEMBL243645

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COc1cc(C(=O)n2nc(C)c(C)c2C)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL243645
Phase Preclinical
Structure Type MOL
InChI Key ZQCWCMVYVBHUNF-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

304.4
MW (Da)
2.52
ALogP
6
HBA
0
HBD
62.6
PSA (Ų)
0.87
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C16H20N2O4
MW 304.35
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.89

Activity Summary

IC50 1 meas. best 5.25
Ki 1 meas. best 4.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 5.25 5.25 5600.0 1
Neutrophil elastase
CHEMBL248
Ki 4.29 4.29 50900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 5600.0 nM 5.25 Inhibition of human pancreatic chymotrypsin 17850059
Neutrophil elastase Ki = 50900.0 nM 4.29 Inhibition of human NE 17850059

Literature References

PubMed DOI Target Context # Activities
17850059 10.1021/jm070600+ Neutrophil elastase 1
17850059 10.1021/jm070600+ Unchecked 1
17850059 10.1021/jm070600+ Aminopeptidase N 1
17850059 10.1021/jm070600+ Cathepsin D 1
17850059 10.1021/jm070600+ Prothrombin 1
17850059 10.1021/jm070600+ Plasma kallikrein 1
17850059 10.1021/jm070600+ Urokinase-type plasminogen activator 1

Data from ChEMBL 36 via Core Engine