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Compound Detail

CHEMBL315211

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COC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NS(=O)(=O)N1CCOCC1)C(=O)N[C@@H](CC1CCCCC1)[C@@H](O)[C@@H](O)CC(C)C

Basic Information

ChEMBL ID CHEMBL315211
Phase Preclinical
Structure Type MOL
InChI Key IEWAGORIVPFRDB-APNLASKRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

654.8
MW (Da)
0.65
ALogP
9
HBA
5
HBD
183.6
PSA (Ų)
0.13
QED
1
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H50N4O9S
MW 654.83
Aromatic Rings 1
Heavy Atoms 45
NP-Likeness -0.09

Activity Summary

IC50 2 meas. best 9.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.55 9.55 0.3 1
Cathepsin D
CHEMBL4106
IC50 7.46 7.46 35.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.28 nM 9.55 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 35.0 nM 7.46 Compound was evaluated for the percent inhibition of Cathepsin D in Bovine 1635057

Literature References

PubMed DOI Target Context # Activities
1635057 10.1021/jm00092a006 Cathepsin D 2
1635057 10.1021/jm00092a006 Renin 1
1635057 10.1021/jm00092a006 Chymotrypsinogen A 1

Data from ChEMBL 36 via Core Engine