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Compound Detail

CHEMBL1818065

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CC(=O)NCCC[C@@](O)(c1cccc(Cl)c1-c1cccc(C)c1)[C@@H]1CCCN(C(=O)[C@H]2C[C@@H](N)[C@@H](O)C2)C1

Basic Information

ChEMBL ID CHEMBL1818065
Phase Preclinical
Structure Type MOL
InChI Key JNRVEYYSIZJHIN-OBVJZYNASA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

542.1
MW (Da)
3.76
ALogP
5
HBA
4
HBD
115.9
PSA (Ų)
0.38
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H40ClN3O4
MW 542.12
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.52

Activity Summary

IC50 1 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

Pharmacokinetic Data

Parameter Value Units Species
T1/2 33.88 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 2.1 nM 8.68 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

Data from ChEMBL 36 via Core Engine