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Compound Detail

CHEMBL2369857

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C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(N)=O

Basic Information

ChEMBL ID CHEMBL2369857
Phase Preclinical
Structure Type MOL
InChI Key WAQIACRLBKOQJK-HNKCEKSGSA-N
1
Targets
6
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

475.6
MW (Da)
-2.14
ALogP
7
HBA
5
HBD
179.3
PSA (Ų)
0.28
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 C23H33N5O6
MW 475.55
Aromatic Rings 1
Heavy Atoms 34
NP-Likeness -0.24

Activity Summary

IC50 6 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytosol aminopeptidase
CHEMBL3965
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytosol aminopeptidase IC50 = 1600.0 nM 5.8 Inhibition against Leucyl aminopeptidase from pig kidney. 10395480

Literature References

PubMed DOI Target Context # Activities
10395480 10.1021/jm9805642 Xaa-Pro aminopeptidase 2 3
10395480 10.1021/jm9805642 Unchecked 2
10395480 10.1021/jm9805642 Xaa-Pro aminopeptidase 1 2
10395480 10.1021/jm9805642 Xaa-Pro dipeptidase 1
10395480 10.1021/jm9805642 Cytosol aminopeptidase 1

Data from ChEMBL 36 via Core Engine