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Compound Detail

CHEMBL2114468

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CC[C@@H](C)[C@@H](S)C(=O)NC1(C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(=O)O)CCCC1

Basic Information

ChEMBL ID CHEMBL2114468
Phase Preclinical
Structure Type MOL
InChI Key OGXZPPQKOPSYNJ-YFXJRYMSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

482.6
MW (Da)
4.24
ALogP
4
HBA
4
HBD
95.5
PSA (Ų)
0.38
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H34N2O4S
MW 482.65
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.21

Activity Summary

IC50 1 meas. best 6.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-converting enzyme 1
CHEMBL4791
IC50 6.39 6.39 410.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-converting enzyme 1 IC50 = 410.0 nM 6.39 In vitro inhibition of human Endothelin converting Enzyme-1 activity 10987444

Literature References

PubMed DOI Target Context # Activities
10987444 10.1016/s0960-894x(00)00403-0 Endothelin-converting enzyme 1 2

Data from ChEMBL 36 via Core Engine