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Compound Detail

CHEMBL256466

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COc1ccc2nc(C(=O)[C@@H](NC(=O)[C@@H]3CCCN3C(=O)[C@@H](NC(=O)c3ccc(C(=O)NS(=O)(=O)c4ccc(Cl)cc4)cc3)C(C)C)C(C)C)oc2c1

Basic Information

ChEMBL ID CHEMBL256466
Phase Preclinical
Structure Type MOL
InChI Key WVLCXRDKCAAKBC-ASVWTAOFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

766.3
MW (Da)
4.38
ALogP
10
HBA
3
HBD
194.1
PSA (Ų)
0.16
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H40ClN5O9S
MW 766.27
Aromatic Rings 4
Heavy Atoms 53
NP-Likeness -0.90

Activity Summary

Ki 1 meas. best 9.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
Ki 9.18 9.18 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase Ki = 0.66 nM 9.18 Inhibition of human neutrophil elastase 18053726

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Neutrophil elastase 1

Data from ChEMBL 36 via Core Engine