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Compound Detail

CHEMBL220389

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O=C(NO)C(Cc1cccc(Oc2ccccc2)c1)C(=O)NCc1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL220389
Phase Preclinical
Structure Type MOL
InChI Key DJLHUFQQCHZLEK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

424.9
MW (Da)
4.11
ALogP
4
HBA
3
HBD
87.7
PSA (Ų)
0.29
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21ClN2O4
MW 424.88
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.65

Activity Summary

IC50 2 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aminopeptidase N
CHEMBL4117
IC50 6.89 6.89 130.0 1
Aminopeptidase N
CHEMBL2590
IC50 5.6 5.6 2527.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aminopeptidase N IC50 = 130.0 nM 6.89 Inhibition of Plasmodium falciparum FcB1 M1 aminopeptidase 17326615
Aminopeptidase N IC50 = 2527.0 nM 5.6 Inhibition of pig kidney microsomal APN 17326615

Literature References

PubMed DOI Target Context # Activities
17326615 10.1021/jm061169b Aminopeptidase N 4

Data from ChEMBL 36 via Core Engine