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Compound Detail

CHEMBL316208

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COc1ccc(C[C@H](NS(=O)(=O)N2CCOCC2)C(=O)N[C@@H](Cc2csc(N)n2)C(=O)N[C@@H](CC2CCCCC2)[C@@H](O)[C@@H](O)CC(C)C)cc1

Basic Information

ChEMBL ID CHEMBL316208
Phase Preclinical
Structure Type MOL
InChI Key QLXHRYKGTCSNKH-STVCLKQXSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

739.0
MW (Da)
1.76
ALogP
11
HBA
6
HBD
205.4
PSA (Ų)
0.13
QED
3
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H54N6O8S2
MW 738.97
Aromatic Rings 2
Heavy Atoms 50
NP-Likeness -0.35

Activity Summary

IC50 2 meas. best 9.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.46 9.46 0.3 1
Cathepsin D
CHEMBL4106
IC50 5.66 5.66 2170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.35 nM 9.46 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 2170.0 nM 5.66 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