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Compound Detail

CHEMBL4092740

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Cl.NCc1ccnc(Oc2cccc(C(=O)N3C[C@H](O)[C@@H](F)C3)c2)c1

Basic Information

ChEMBL ID CHEMBL4092740
Phase Preclinical
Structure Type MOL
InChI Key BKRZYDXKJLEFCP-YYLIZZNMSA-N
Parent Compound CHEMBL4118001
Active Moiety CHEMBL4118001
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

331.4
MW (Da)
1.49
ALogP
5
HBA
2
HBD
88.7
PSA (Ų)
0.89
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 C17H19ClFN3O3
MW 367.81
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.17

Activity Summary

IC50 5 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysyl oxidase homolog 2
CHEMBL3714029
IC50 7.09 6.65 82.0 3
Lysyl oxidase homolog 3
CHEMBL4105989
IC50 5.91 5.91 1220.0 1
Protein-lysine 6-oxidase
CHEMBL2249
IC50 4.28 4.28 52000.0 1

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 5
28471663 10.1021/acs.jmedchem.7b00345 Protein-lysine 6-oxidase 1
28471663 10.1021/acs.jmedchem.7b00345 Lysyl oxidase homolog 3 1
28471663 10.1021/acs.jmedchem.7b00345 Amine oxidase [copper-containing] 3 1
28471663 10.1021/acs.jmedchem.7b00345 Diamine oxidase [copper-containing] 1
28471663 10.1021/acs.jmedchem.7b00345 Amine oxidase [flavin-containing] A 1
28471663 10.1021/acs.jmedchem.7b00345 Amine oxidase [flavin-containing] B 1
28471663 10.1021/acs.jmedchem.7b00345 Unchecked 1

Data from ChEMBL 36 via Core Engine