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Compound Detail

CHEMBL25221

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CC(C)C(CP(=O)([O-])C(Cc1ccccc1)NC(=O)[C@H](CCCCNC(=O)OCc1ccccc1)NS(C)(=O)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)[O-].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL25221
Phase Preclinical
Structure Type MOL
InChI Key ZYRMWYJAAUFQQS-KHSQIVFISA-L
Parent Compound CHEMBL1204798
Active Moiety CHEMBL1204798
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

825.9
MW (Da)
4.52
ALogP
8
HBA
7
HBD
233.1
PSA (Ų)
0.04
QED
2
Ro5 Violations
22
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H50N5Na2O10PS
MW 869.89
Aromatic Rings 4
Heavy Atoms 57
NP-Likeness -0.14

Activity Summary

IC50 1 meas. best 6.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-converting enzyme 1
CHEMBL4791
IC50 6.41 6.41 390.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-converting enzyme 1 IC50 = 390.0 nM 6.41 Inhibition of Endothelin-converting enzyme of guinea pig lung membrane -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00211-9 Endothelin-converting enzyme 1 1
- 10.1016/0960-894X(96)00211-9 Neprilysin 1

Data from ChEMBL 36 via Core Engine