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Compound Detail

CHEMBL59887

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CCN1C[C@@H]([C@H](O)[C@H](CC2CCCCC2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CC(=O)N2C[C@H](OCOC)[C@H](OCOC)C2)Cc2ccccc2)OC1=O

Basic Information

ChEMBL ID CHEMBL59887
Phase Preclinical
Structure Type MOL
InChI Key XDZOMKZUBUHOHZ-MSXNJZMTSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

770.9
MW (Da)
2.16
ALogP
11
HBA
4
HBD
193.9
PSA (Ų)
0.14
QED
2
Ro5 Violations
21
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H58N6O10
MW 770.92
Aromatic Rings 2
Heavy Atoms 55
NP-Likeness 0.19

Activity Summary

IC50 2 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.57 8.265 2.7 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.7 nM 8.57 Inhibitory activity against purified human renal renin at pH 6.5 2194033
Renin IC50 = 11.0 nM 7.96 Inhibitory activity against human plasma renin at pH 7.4 2194033

Literature References

PubMed DOI Target Context # Activities
2194033 10.1021/jm00169a024 No relevant target 3
2194033 10.1021/jm00169a024 Renin 2

Data from ChEMBL 36 via Core Engine