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Compound Detail

CHEMBL163454

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O=C(N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)O)[C@H](S)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL163454
Phase Preclinical
Structure Type MOL
InChI Key BNECOBGISSOLPT-FCHUYYIVSA-N
6
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
4.01
ALogP
3
HBA
3
HBD
66.4
PSA (Ų)
0.50
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23NO3S
MW 405.52
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.12

Activity Summary

Ki 4 meas. best 8.89
IC50 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL1944
Ki 8.89 8.89 1.3 1
Neprilysin
CHEMBL3369
IC50 7.0 7.0 100.0 1
Carboxypeptidase A1
CHEMBL2088
Ki 6.51 6.51 310.0 1
Angiotensin-converting enzyme
CHEMBL1808
Ki 6.28 6.28 520.0 1
Angiotensin-converting enzyme
CHEMBL2096989
IC50 6.16 6.16 688.0 1
Angiotensin-converting enzyme 2
CHEMBL3736
Ki 5.85 5.85 1400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00105-3 Angiotensin-converting enzyme 1
- 10.1016/0960-894X(95)00105-3 Neprilysin 1
18078750 10.1016/j.bmcl.2007.11.048 Angiotensin-converting enzyme 2 1
18078750 10.1016/j.bmcl.2007.11.048 Angiotensin-converting enzyme 1
18078750 10.1016/j.bmcl.2007.11.048 Neprilysin 1
18078750 10.1016/j.bmcl.2007.11.048 Carboxypeptidase A1 1

Data from ChEMBL 36 via Core Engine