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Compound Detail

CHEMBL60363

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CN(C)c1ccc2c(c1)CCC2C(CS)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O

Basic Information

ChEMBL ID CHEMBL60363
Phase Preclinical
Structure Type MOL
InChI Key MRVQIUAKKUQTTP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

451.6
MW (Da)
3.62
ALogP
4
HBA
4
HBD
85.4
PSA (Ų)
0.39
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 C25H29N3O3S
MW 451.59
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 0.06

Activity Summary

Ki 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neprilysin
CHEMBL3768
Ki 7.82 7.82 15.0 1
Angiotensin-converting enzyme
CHEMBL2625
Ki 7.36 7.36 44.0 1
Endothelin-converting enzyme 1
CHEMBL4791
Ki 6.43 6.43 370.0 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