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Compound Detail

CHEMBL4862937

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NCc1cccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2ccc(C(OCC3CC3)c3ccccc3)cc2F)c1

Basic Information

ChEMBL ID CHEMBL4862937
Phase Preclinical
Structure Type MOL
InChI Key HBXVQXKJLUQKAE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

538.5
MW (Da)
6.26
ALogP
5
HBA
2
HBD
82.2
PSA (Ų)
0.25
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H26F4N4O2
MW 538.55
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.46

Activity Summary

IC50 1 meas. best 6.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
IC50 6.19 6.19 651.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein IC50 = 651.0 nM 6.19 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