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Compound Detail

CHEMBL431217

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CCOC(=O)C(F)(F)C(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](Cc1csc(N)n1)NC(=O)[C@H](Cc1ccccc1)NS(=O)(=O)N1CCOCC1

Basic Information

ChEMBL ID CHEMBL431217
Phase Preclinical
Structure Type MOL
InChI Key ZEYSVLZKQXCERB-GSDHBNRESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

742.9
MW (Da)
1.75
ALogP
11
HBA
4
HBD
199.1
PSA (Ų)
0.14
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H44F2N6O8S2
MW 742.87
Aromatic Rings 2
Heavy Atoms 50
NP-Likeness -0.75

Activity Summary

IC50 2 meas. best 9.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.27 9.27 0.5 1
Cathepsin D
CHEMBL4106
IC50 5.19 5.19 6400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.54 nM 9.27 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 6400.0 nM 5.19 Inhibition of Bovine Cathepsin D 1635057

Literature References

PubMed DOI Target Context # Activities
1635057 10.1021/jm00092a006 Renin 1
1635057 10.1021/jm00092a006 Cathepsin D 1
1635057 10.1021/jm00092a006 Unchecked 1

Data from ChEMBL 36 via Core Engine