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Compound Detail

CHEMBL398168

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O=C(c1c(F)cccc1F)n1cc(Br)cn1

Basic Information

ChEMBL ID CHEMBL398168
Phase Preclinical
Structure Type MOL
InChI Key PZQVUIJLKBCLOG-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

287.1
MW (Da)
2.61
ALogP
3
HBA
0
HBD
34.9
PSA (Ų)
0.81
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H5BrF2N2O
MW 287.06
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -1.72

Activity Summary

IC50 2 meas. best 5.75
Ki 1 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
Ki 5.96 5.96 1100.0 1
Unchecked
CHEMBL612545
IC50 5.75 5.75 1800.0 1
Urokinase-type plasminogen activator
CHEMBL3286
IC50 4.49 4.49 32300.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 3.1 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase Ki = 1100.0 nM 5.96 Inhibition of human NE 17850059
Unchecked IC50 = 1800.0 nM 5.75 Inhibition of human pancreatic chymotrypsin 17850059
Urokinase-type plasminogen activator IC50 = 32300.0 nM 4.49 Inhibition of human urokinase 17850059

Literature References

PubMed DOI Target Context # Activities
17850059 10.1021/jm070600+ Neutrophil elastase 1
17850059 10.1021/jm070600+ No relevant target 1
17850059 10.1021/jm070600+ Unchecked 1
17850059 10.1021/jm070600+ Urokinase-type plasminogen activator 1
17850059 10.1021/jm070600+ Aminopeptidase N 1
17850059 10.1021/jm070600+ Cathepsin D 1
17850059 10.1021/jm070600+ Plasma kallikrein 1
17850059 10.1021/jm070600+ Prothrombin 1

Data from ChEMBL 36 via Core Engine