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Compound Detail

CHEMBL61016

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CSc1ccc2c(c1)CCC2C(CS)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O

Basic Information

ChEMBL ID CHEMBL61016
Phase Preclinical
Structure Type MOL
InChI Key VDSMHDIVRBRETF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

454.6
MW (Da)
4.28
ALogP
4
HBA
4
HBD
82.2
PSA (Ų)
0.30
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 C24H26N2O3S2
MW 454.62
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 0.02

Activity Summary

Ki 3 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL3768
Ki 8.22 8.22 6.0 1
Angiotensin-converting enzyme
CHEMBL2625
Ki 7.85 7.85 14.0 1
Endothelin-converting enzyme 1
CHEMBL4791
Ki 7.46 7.46 35.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12113828 10.1016/s0960-894x(02)00248-2 Neprilysin 1
12113828 10.1016/s0960-894x(02)00248-2 Angiotensin-converting enzyme 1
12113828 10.1016/s0960-894x(02)00248-2 Endothelin-converting enzyme 1 1

Data from ChEMBL 36 via Core Engine