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Compound Detail

CHEMBL1818068

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CCc1cccc(-c2c(F)cccc2[C@](O)(CCCCOC)[C@H]2CN(C(=O)[C@H]3C[C@@H](N)[C@@H](O)C3)CCO2)c1

Basic Information

ChEMBL ID CHEMBL1818068
Phase Preclinical
Structure Type MOL
InChI Key GINXSGVWXWGOTE-QHXQRBBOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

528.7
MW (Da)
3.39
ALogP
6
HBA
3
HBD
105.2
PSA (Ų)
0.41
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H41FN2O5
MW 528.67
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.6 8.6 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.5 nM 8.6 Inhibition of recombinant human renin using of DABCYL-c-Abu-IleHis-Pro-Phe-His-L... 21741239

Literature References

PubMed DOI Target Context # Activities
21741239 10.1016/j.bmcl.2011.06.043 Renin 2
21741239 10.1016/j.bmcl.2011.06.043 Cytochrome P450 3A4 1
21741239 10.1016/j.bmcl.2011.06.043 Beta-secretase 1 1
21741239 10.1016/j.bmcl.2011.06.043 Cathepsin D 1
21741239 10.1016/j.bmcl.2011.06.043 Cathepsin E 1

Data from ChEMBL 36 via Core Engine