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Compound Detail

CHEMBL292677

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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)C(=O)NC(Cc1c[nH]cn1)C(=O)O

Basic Information

ChEMBL ID CHEMBL292677
Phase Preclinical
Structure Type MOL
InChI Key LCGRSLFZYGRZGX-BDTNELKKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

777.9
MW (Da)
0.01
ALogP
10
HBA
8
HBD
252.4
PSA (Ų)
0.08
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H55N7O10S
MW 777.94
Aromatic Rings 2
Heavy Atoms 54
NP-Likeness -0.07

Activity Summary

IC50 2 meas. best 9.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.64 9.64 0.2 1
Cathepsin D
CHEMBL4106
IC50 4.29 4.29 51800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.23 nM 9.64 Inhibition of monkey plasma renin 2066966
Cathepsin D IC50 = 51800.0 nM 4.29 Inhibitory concentration on Bovine Cathepsin D 2066966

Literature References

PubMed DOI Target Context # Activities
2066966 10.1021/jm00111a002 Renin 1
2066966 10.1021/jm00111a002 Cathepsin D 1
2066966 10.1021/jm00111a002 Monkey 1

Data from ChEMBL 36 via Core Engine