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Compound Detail

CHEMBL420417

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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)NC(=O)OC(C)(C)C

Basic Information

ChEMBL ID CHEMBL420417
Phase Preclinical
Structure Type MOL
InChI Key MNCJMPPTISDLKZ-MYHRABSESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

659.9
MW (Da)
4.11
ALogP
9
HBA
6
HBD
175.9
PSA (Ų)
0.17
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H53N5O6S
MW 659.89
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness -0.05

Activity Summary

IC50 2 meas. best 8.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.63 8.63 2.3 1
Cathepsin D
CHEMBL4106
IC50 6.12 6.12 763.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.34 nM 8.63 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 763.0 nM 6.12 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