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Compound Detail

CHEMBL570740

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O=C(N[C@@H](Cc1ccccc1)P(=O)(O)CC(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL570740
Phase Preclinical
Structure Type MOL
InChI Key ICSDSFFBTUMVKX-UQLRSZRFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

743.8
MW (Da)
7.57
ALogP
5
HBA
5
HBD
157.8
PSA (Ų)
0.06
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H42N3O7P
MW 743.80
Aromatic Rings 6
Heavy Atoms 54
NP-Likeness -0.06

Activity Summary

Ki 2 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiotensin-converting enzyme
CHEMBL1808
Ki 7.92 7.92 12.0 1
Neprilysin
CHEMBL1944
Ki 7.28 7.28 52.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiotensin-converting enzyme Ki = 12.0 nM 7.92 Inhibition of human somatic ACE C-terminal domain 19899765
Neprilysin Ki = 52.0 nM 7.28 Inhibition of human somatic NEP 19899765

Literature References

PubMed DOI Target Context # Activities
19899765 10.1021/jm9010803 Angiotensin-converting enzyme 1
19899765 10.1021/jm9010803 Neprilysin 1
19899765 10.1021/jm9010803 Endothelin-converting enzyme 1 1

Data from ChEMBL 36 via Core Engine