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Compound Detail

CHEMBL84195

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O=C(O)c1ccc(NC(=O)[C@@H](Cc2ccccc2)C[C@H](Cc2ccccc2)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL84195
Phase Preclinical
Structure Type MOL
InChI Key MTIKEXSWCQTDKS-VXKWHMMOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

431.5
MW (Da)
4.52
ALogP
3
HBA
3
HBD
103.7
PSA (Ų)
0.44
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 C26H25NO5
MW 431.49
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.29

Activity Summary

IC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL3369
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neprilysin IC50 = 800.0 nM 6.1 Inhibition of enkephalinase activity in synaptic membranes prepared from rat str... 2585440

Literature References

PubMed DOI Target Context # Activities
2585440 10.1021/jm00132a005 Neprilysin 1

Data from ChEMBL 36 via Core Engine