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Compound Detail

CHEMBL5661839

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CCOC(=O)C1=C(N)N(c2cccc([N+](=O)[O-])c2)C(C)=C(C(C)=O)C1c1ccc(Br)cc1

Basic Information

ChEMBL ID CHEMBL5661839
Phase Preclinical
Structure Type MOL
InChI Key IUWVDURXQOYQEP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

500.4
MW (Da)
4.56
ALogP
7
HBA
1
HBD
115.8
PSA (Ų)
0.35
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22BrN3O5
MW 500.35
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.22

Activity Summary

IC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
IC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase IC50 = 200.0 nM 6.7 Inhibition of human neutrophil elastase using MeOSuc-AAPV-MCA as substrate measu... 26083237

Literature References

PubMed DOI Target Context # Activities
26083237 10.1002/cmdc.201500131 Neutrophil elastase 1
26083237 10.1002/cmdc.201500131 ADMET 1

Data from ChEMBL 36 via Core Engine