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Compound Detail

CHEMBL418841

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CC(=O)Nc1ccc(-c2ccccc2)n(CC(=O)NC(C(=O)C(F)(F)F)C(C)C)c1=O

Basic Information

ChEMBL ID CHEMBL418841
Phase Preclinical
Structure Type MOL
InChI Key QPCWIYWAIOFNGK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

437.4
MW (Da)
2.75
ALogP
5
HBA
2
HBD
97.3
PSA (Ų)
0.70
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22F3N3O4
MW 437.42
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.02

Activity Summary

Ki 1 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
Ki 7.24 7.24 57.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 6353.16 nM Cricetinae
F 35.0 % Cricetulus griseus
T1/2 1.9 hr Cricetinae
Tmax 0.25 hr Cricetinae

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase Ki = 57.0 nM 7.24 Binding affinity against human leukocyte elastase (HLE) enzyme 7932559

Literature References

PubMed DOI Target Context # Activities
7932559 10.1021/jm00046a016 No relevant target 3
7932559 10.1021/jm00046a016 Hamster 3
7932559 10.1021/jm00046a016 Cricetinae gen. sp. 2
7932559 10.1021/jm00046a016 Neutrophil elastase 1
7932559 10.1021/jm00046a016 ADMET 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine