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Compound Detail

CHEMBL1818066

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COCCCC[C@@](O)(c1cccc(F)c1-c1cccc(C)c1)[C@H]1CN(C(=O)[C@H]2C[C@@H](N)[C@@H](O)C2)CCO1

Basic Information

ChEMBL ID CHEMBL1818066
Phase Preclinical
Structure Type MOL
InChI Key SCFOYWHZASHDOQ-RWNGQHIQSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

514.6
MW (Da)
3.13
ALogP
6
HBA
3
HBD
105.2
PSA (Ų)
0.44
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39FN2O5
MW 514.64
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness -0.39

Activity Summary

IC50 1 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.42 8.42 3.8 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.65 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 3.8 nM 8.42 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 Liver microsomes 1
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