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Compound Detail

CHEMBL86374

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

Basic Information

ChEMBL ID CHEMBL86374
Phase Preclinical
Structure Type MOL
InChI Key QGJKHQRFJGLJLV-PBIKNJLJSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

709.0
MW (Da)
1.75
ALogP
10
HBA
6
HBD
196.2
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 C33H52N6O7S2
MW 708.95
Aromatic Rings 2
Heavy Atoms 48
NP-Likeness -0.37

Activity Summary

IC50 2 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 7.48 7.48 33.0 1
Cathepsin D
CHEMBL4106
IC50 4.84 4.84 14500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 33.0 nM 7.48 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 14500.0 nM 4.84 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