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Compound Detail

CHEMBL3221965

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CC(C)C[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)O

Basic Information

ChEMBL ID CHEMBL3221965
Phase Preclinical
Structure Type MOL
InChI Key PBKZFAANHLYJOZ-YUMQZZPRSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

261.3
MW (Da)
-0.31
ALogP
4
HBA
4
HBD
123.9
PSA (Ų)
0.47
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 C11H19NO6
MW 261.27
Aromatic Rings 0
Heavy Atoms 18
NP-Likeness 0.63

Activity Summary

IC50 1 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL1944
IC50 7.2 7.2 63.1 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 24.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neprilysin IC50 = 63.1 nM 7.2 Inhibition of human NEP using N-Dansyl-D-Ala-Gly-p-nitro-Phe-Gly as substrate pr... -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C2MD00287F No relevant target 2
- 10.1039/C2MD00287F Neprilysin 1
- 10.1039/C2MD00287F Endothelin-converting enzyme 1 1
- 10.1039/C2MD00287F Angiotensin-converting enzyme 1
- 10.1039/C2MD00287F Plasma 1
- 10.1039/C2MD00287F ADMET 1

Data from ChEMBL 36 via Core Engine