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Compound Detail

CHEMBL4081837

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NCc1cc(O[C@@H]2CCCN(C(=O)Nc3ccccc3)C2)nc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL4081837
Phase Preclinical
Structure Type MOL
InChI Key NPNATZWDBSJWKE-OAHLLOKOSA-N
1
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

394.4
MW (Da)
3.63
ALogP
4
HBA
2
HBD
80.5
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21F3N4O2
MW 394.40
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.49

Activity Summary

IC50 3 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysyl oxidase homolog 2
CHEMBL3714029
IC50 6.24 5.6167 570.0 3

Pharmacokinetic Data

Parameter Value Units Species
Cmax - - Mus musculus
Cmax - - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28471663 10.1021/acs.jmedchem.7b00345 Lysyl oxidase homolog 2 3
28471663 10.1021/acs.jmedchem.7b00345 Protein-lysine 6-oxidase 1
28471663 10.1021/acs.jmedchem.7b00345 Lung 1
28471663 10.1021/acs.jmedchem.7b00345 Plasma 1

Data from ChEMBL 36 via Core Engine