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Compound Detail

CHEMBL571153

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

Basic Information

ChEMBL ID CHEMBL571153
Phase Preclinical
Structure Type MOL
InChI Key WWTBZEKOSBFBEM-SPWPXUSOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

667.7
MW (Da)
5.90
ALogP
5
HBA
5
HBD
157.8
PSA (Ų)
0.09
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H38N3O7P
MW 667.70
Aromatic Rings 5
Heavy Atoms 48
NP-Likeness -0.02

Activity Summary

Ki 2 meas. best 8.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-converting enzyme 1
CHEMBL4791
Ki 8.92 8.92 1.2 1
Neprilysin
CHEMBL1944
Ki 8.85 8.85 1.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-converting enzyme 1 Ki = 1.2 nM 8.92 Inhibition of human somatic ECE1 19899765
Neprilysin Ki = 1.4 nM 8.85 Inhibition of human somatic NEP 19899765

Literature References

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

Data from ChEMBL 36 via Core Engine