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Compound Detail

CHEMBL4867482

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CS(=O)(=O)c1cccc(-c2ccc(NC(=O)c3cc(C(F)(F)F)nn3-c3cccc(CN)c3)c(F)c2)c1

Basic Information

ChEMBL ID CHEMBL4867482
Phase Preclinical
Structure Type MOL
InChI Key JFZYZNSMVHQKCJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

532.5
MW (Da)
4.81
ALogP
6
HBA
2
HBD
107.1
PSA (Ų)
0.35
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20F4N4O3S
MW 532.52
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.87

Activity Summary

IC50 1 meas. best 5.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
IC50 5.91 5.91 1229.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein IC50 = 1229.0 nM 5.91 Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as... 34436898

Literature References

PubMed DOI Target Context # Activities
34436898 10.1021/acs.jmedchem.1c00511 Plasma kallikrein 1

Data from ChEMBL 36 via Core Engine