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Compound Detail

CHEMBL267955

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CCCOC(NC(=O)[C@H](Cc1ccccc1)NS(=O)(=O)N1CCOCC1)C(=O)N[C@@H](CC1CCCCC1)C(=O)C(F)(F)C(=O)NCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL267955
Phase Preclinical
Structure Type MOL
InChI Key QUSCBNSWNRTFJQ-QXSWOPKKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

772.9
MW (Da)
0.74
ALogP
10
HBA
4
HBD
184.7
PSA (Ų)
0.11
QED
1
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H54F2N6O9S
MW 772.91
Aromatic Rings 1
Heavy Atoms 53
NP-Likeness -0.78

Activity Summary

IC50 2 meas. best 8.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.68 8.68 2.1 1
Cathepsin D
CHEMBL4106
IC50 6.88 6.88 131.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.1 nM 8.68 Inhibitory activity against monkey renin in vitro. 1552498
Cathepsin D IC50 = 131.0 nM 6.88 Inhibitory activity against bovine cathepsin D 1552498

Literature References

PubMed DOI Target Context # Activities
1552498 10.1021/jm00084a008 Monkey 3
1552498 10.1021/jm00084a008 Renin 1
1552498 10.1021/jm00084a008 Cathepsin D 1
1552498 10.1021/jm00084a008 Unchecked 1

Data from ChEMBL 36 via Core Engine