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Compound Detail

CHEMBL43370

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CS(=O)(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)P(=O)(O)CC1(C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)CCCC1

Basic Information

ChEMBL ID CHEMBL43370
Phase Preclinical
Structure Type MOL
InChI Key UBQFBYMIHFXWBF-YTCPBCGMSA-N
6
Targets
9
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

703.8
MW (Da)
2.84
ALogP
7
HBA
7
HBD
220.8
PSA (Ų)
0.08
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H46N5O8PS
MW 703.80
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness 0.04

Activity Summary

IC50 9 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiotensin-converting enzyme
CHEMBL1808
IC50 8.6 8.6 2.5 1
Angiotensin-converting enzyme
CHEMBL2625
IC50 8.6 8.6 2.5 2
Endothelin-converting enzyme 1
CHEMBL4791
IC50 7.16 7.12 70.0 3
Neprilysin
CHEMBL1944
IC50 7.05 7.05 90.0 1
Neprilysin
CHEMBL3369
IC50 7.05 7.05 90.0 1
Neprilysin
CHEMBL3768
IC50 7.05 7.05 90.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00297-1 Endothelin-converting enzyme 1 1
- 10.1016/0960-894X(96)00297-1 Angiotensin-converting enzyme 1
- 10.1016/0960-894X(96)00297-1 Neprilysin 1
11906289 10.1021/jm0005454 Neprilysin 1
11906289 10.1021/jm0005454 Angiotensin-converting enzyme 1
11906289 10.1021/jm0005454 Endothelin-converting enzyme 1 1
19899765 10.1021/jm9010803 Angiotensin-converting enzyme 1
19899765 10.1021/jm9010803 Endothelin-converting enzyme 1 1
19899765 10.1021/jm9010803 Neprilysin 1

Data from ChEMBL 36 via Core Engine