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Compound Detail

CHEMBL3617972

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CC1=C(C#N)[C@@H](c2ccc(C#N)cc2S(C)(=O)=O)NC(=O)N1c1cccc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL3617972
Phase Preclinical
Structure Type MOL
InChI Key WQASVWJQEKONLG-LJQANCHMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

460.4
MW (Da)
4.05
ALogP
5
HBA
1
HBD
114.1
PSA (Ų)
0.74
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H15F3N4O3S
MW 460.44
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.60

Activity Summary

IC50 1 meas. best 9.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
IC50 9.27 9.27 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase IC50 = 0.54 nM 9.27 Inhibition of human neutrophil elastase using MeOSuc-AAPV-MCA as substrate measu... 26083237

Literature References

PubMed DOI Target Context # Activities
26358162 10.1016/j.bmcl.2015.08.049 Neutrophil elastase 1
26083237 10.1002/cmdc.201500131 Neutrophil elastase 1
26083237 10.1002/cmdc.201500131 Cytochrome P450 2C9 1
26083237 10.1002/cmdc.201500131 Cytochrome P450 3A4 1
26083237 10.1002/cmdc.201500131 No relevant target 1

Data from ChEMBL 36 via Core Engine