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Compound Detail

CHEMBL441325

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CC(C)C[C@H](O)[C@H](O)[C@H](CC1CCCCC1)NC(=O)C(NC(=O)[C@H](Cc1ccccc1)NS(=O)(=O)N1CCOCC1)OCC(F)(F)F

Basic Information

ChEMBL ID CHEMBL441325
Phase Preclinical
Structure Type MOL
InChI Key OLVKUCXGMNZXGZ-JXSHCWFBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

694.8
MW (Da)
2.01
ALogP
8
HBA
5
HBD
166.5
PSA (Ų)
0.15
QED
1
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H49F3N4O8S
MW 694.81
Aromatic Rings 1
Heavy Atoms 47
NP-Likeness -0.32

Activity Summary

IC50 2 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.74 9.74 0.2 1
Cathepsin D
CHEMBL4106
IC50 7.67 7.67 21.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.18 nM 9.74 Inhibitory activity against monkey renin in vitro. 1552498
Cathepsin D IC50 = 21.2 nM 7.67 Inhibitory activity against bovine cathepsin D 1552498

Literature References

PubMed DOI Target Context # Activities
1552498 10.1021/jm00084a008 Monkey 3
1552498 10.1021/jm00084a008 Renin 1
1552498 10.1021/jm00084a008 Cathepsin D 1
1552498 10.1021/jm00084a008 Unchecked 1

Data from ChEMBL 36 via Core Engine