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Compound Detail

CHEMBL1818063

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COC(=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 CHEMBL1818063
Phase Preclinical
Structure Type MOL
InChI Key XMFPYLMRYFHYBN-YWHUKLHMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

558.1
MW (Da)
3.98
ALogP
6
HBA
4
HBD
125.1
PSA (Ų)
0.36
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 C30H40ClN3O5
MW 558.12
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.52

Activity Summary

IC50 1 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 8.96 8.96 1.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 1.1 nM 8.96 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

Data from ChEMBL 36 via Core Engine