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Compound Detail

CHEMBL85672

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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)NP(=O)(OC(C)C)OC(C)C

Basic Information

ChEMBL ID CHEMBL85672
Phase Preclinical
Structure Type MOL
InChI Key IKQAPARFDOBBMW-QEUNAIBPSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

723.9
MW (Da)
5.13
ALogP
10
HBA
6
HBD
185.1
PSA (Ų)
0.10
QED
3
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H58N5O7PS
MW 723.92
Aromatic Rings 2
Heavy Atoms 49
NP-Likeness 0.10

Activity Summary

IC50 2 meas. best 9.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.04 9.04 0.9 1
Cathepsin D
CHEMBL4106
IC50 7.48 7.48 33.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 0.91 nM 9.04 In vitro inhibition of monkey renin. 1635057
Cathepsin D IC50 = 33.0 nM 7.48 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

Data from ChEMBL 36 via Core Engine