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Compound Detail

CHEMBL90388

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O=CN(O)C[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCc2ccccc2N(CC(=O)O)C1=O

Basic Information

ChEMBL ID CHEMBL90388
Phase Preclinical
Structure Type MOL
InChI Key VJMGHCZAAFBQOG-MOPGFXCFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
1.24
ALogP
5
HBA
3
HBD
127.2
PSA (Ų)
0.31
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25N3O6
MW 439.47
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.33

Activity Summary

IC50 2 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL3369
IC50 8.89 8.89 1.3 1
Angiotensin-converting enzyme
CHEMBL4074
IC50 8.28 8.28 5.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neprilysin IC50 = 1.3 nM 8.89 Inhibition of Neutral endopeptidase 10698448
Angiotensin-converting enzyme IC50 = 5.3 nM 8.28 Inhibition of Angiotensin I converting enzyme 10698448

Literature References

PubMed DOI Target Context # Activities
10698448 10.1016/s0960-894x(99)00671-x Angiotensin-converting enzyme 1
10698448 10.1016/s0960-894x(99)00671-x Neprilysin 1

Data from ChEMBL 36 via Core Engine