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Compound Detail

CHEMBL5594679

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CCCNC(=O)Nc1cccc(S(=O)(=O)Nc2cccc([C@@H](CC(=O)[O-])NC(=O)Nc3ccc(NC(=O)NCCOCCOCCOCCC(=O)N[C@@H](CC(=O)[O-])C(=O)N4CCC[C@H]4C(=O)N[C@H](C(=O)O[C@]4(CC)C(=O)OCc5c4cc4n(c5=O)Cc5c-4nc4ccccc4c5CC)C(C)C)cc3)c2)c1.[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL5594679
Phase Preclinical
Structure Type MOL
InChI Key ZVBHCHRVKCGYDA-YBUSIOMQSA-L
Parent Compound CHEMBL6068064
Active Moiety CHEMBL6068064
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

1471.6
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C72H84N12Na2O20S
MW 1515.57

Activity Summary

IC50 2 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL5156
IC50 5.05 5.05 8900.0 1
Neutrophil elastase
CHEMBL248
IC50 5.02 5.02 9600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase IC50 = 8900.0 nM 5.05 Inhibition of mouse Neutrophil elastase 38421819
Neutrophil elastase IC50 = 9600.0 nM 5.02 Inhibition of human Neutrophil elastase 38421819

Literature References

PubMed DOI Target Context # Activities
38421819 10.1021/acs.jmedchem.3c02115 Neutrophil elastase 2
38421819 10.1021/acs.jmedchem.3c02115 ADMET 2

Data from ChEMBL 36 via Core Engine