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Compound Detail

CHEMBL403896

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CC(C)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)O)[C@H](C)OC(=O)CC[C@@H]2NC(=O)[C@@H]3COC(=O)C[C@H](NC(=O)[C@H](Cc4cc5ccccc5[nH]4)NC2=O)C(=O)N[C@H](C(=O)O)CC(=O)NCCCC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N3

Basic Information

ChEMBL ID CHEMBL403896
Phase Preclinical
Structure Type MOL
InChI Key OBJRDBYSSAEARM-WSFPPIIISA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

1284.4
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C61H81N13O18
MW 1284.39

Activity Summary

IC50 1 meas. best 6.57
Ki 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
Ki 8.0 8.0 10.0 1
Pancreatic elastase
CHEMBL2096984
IC50 6.57 6.57 270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase Ki = 10.0 nM 8.0 Inhibition of human leukocyte elastase 17470393
Pancreatic elastase IC50 = 270.0 nM 6.57 Inhibition of porcine pancreatic elastase 17470393

Literature References

PubMed DOI Target Context # Activities
17470393 10.1016/j.bmc.2007.03.082 Pancreatic elastase 1
17470393 10.1016/j.bmc.2007.03.082 Neutrophil elastase 1

Data from ChEMBL 36 via Core Engine