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Compound Detail

CHEMBL423635

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O=C(N[C@@H](Cc1ccc2ccccc2c1)C(=O)N1CCC[C@H]1C(=O)O)[C@@H](S)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL423635
Phase Preclinical
Structure Type MOL
InChI Key NKBFLPNYTZKMLW-HJOGWXRNSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
3.48
ALogP
4
HBA
3
HBD
86.7
PSA (Ų)
0.43
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 C27H28N2O4S
MW 476.60
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.19

Activity Summary

IC50 2 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Angiotensin-converting enzyme
CHEMBL2096989
IC50 7.75 7.75 18.0 1
Neprilysin
CHEMBL3369
IC50 6.15 6.15 705.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Angiotensin-converting enzyme IC50 = 18.0 nM 7.75 Inhibition of angiotensin converting enzyme (ACE) -
Neprilysin IC50 = 705.0 nM 6.15 Inhibition of neutral endopeptidase (NEP) 24.11 -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00105-3 Rattus norvegicus 2
- 10.1016/0960-894X(95)00105-3 Angiotensin-converting enzyme 1
- 10.1016/0960-894X(95)00105-3 Neprilysin 1

Data from ChEMBL 36 via Core Engine