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Compound Detail

CHEMBL28311

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O=C(N[C@@H](CC1CCCCC1)C(O)C(F)(F)C(=O)NCCN1CCOCC1)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NS(=O)(=O)N1CCOCC1

Basic Information

ChEMBL ID CHEMBL28311
Phase Preclinical
Structure Type MOL
InChI Key BVPCJACDNLTJEX-WDJCGXDUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

796.9
MW (Da)
0.11
ALogP
10
HBA
6
HBD
207.3
PSA (Ų)
0.11
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H54F2N8O8S
MW 796.94
Aromatic Rings 2
Heavy Atoms 55
NP-Likeness -0.66

Activity Summary

IC50 1 meas. best 8.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.53 8.53 3.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.96 nM 8.53 The concentration producing 50% inhibition of renin activity in monkey plasma wa... 1732531

Literature References

PubMed DOI Target Context # Activities
1732531 10.1021/jm00079a001 Renin 1
1732531 10.1021/jm00079a001 Cathepsin D 1
1732531 10.1021/jm00079a001 Unchecked 1

Data from ChEMBL 36 via Core Engine