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Compound Detail

CHEMBL161879

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CC(C)[C@H](S)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CO)C(=O)O

Basic Information

ChEMBL ID CHEMBL161879
Phase Preclinical
Structure Type MOL
InChI Key DVYQZBMHVMYYAF-UFYCRDLUSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

444.6
MW (Da)
1.90
ALogP
5
HBA
5
HBD
115.7
PSA (Ų)
0.36
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28N2O5S
MW 444.55
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 0.12

Activity Summary

IC50 2 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL3369
IC50 7.37 7.37 43.0 1
Angiotensin-converting enzyme
CHEMBL2096989
IC50 7.0 7.0 100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neprilysin IC50 = 43.0 nM 7.37 Inhibition of neutral endopeptidase (NEP) 24.11 -
Angiotensin-converting enzyme IC50 = 100.0 nM 7.0 Inhibition of angiotensin converting enzyme (ACE) -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00105-3 Angiotensin-converting enzyme 1
- 10.1016/0960-894X(95)00105-3 Neprilysin 1

Data from ChEMBL 36 via Core Engine