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Compound Detail

CHEMBL230261

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CCc1nc(N)nc(N)c1-c1ccc2c(c1)N(CCCC(=O)OC)CCC2

Basic Information

ChEMBL ID CHEMBL230261
Phase Preclinical
Structure Type MOL
InChI Key CQONVFYJFFOPQX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

369.5
MW (Da)
2.58
ALogP
7
HBA
2
HBD
107.4
PSA (Ų)
0.75
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27N5O2
MW 369.47
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 6.92 6.92 120.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.08333 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 120.0 nM 6.92 Inhibition of renin 17482464

Literature References

PubMed DOI Target Context # Activities
17482464 10.1016/j.bmcl.2007.04.052 Renin 1
17482464 10.1016/j.bmcl.2007.04.052 Cytochrome P450 3A4 1
17482464 10.1016/j.bmcl.2007.04.052 Liver microsomes 1
17482464 10.1016/j.bmcl.2007.04.052 Cathepsin D 1
17482464 10.1016/j.bmcl.2007.04.052 Cathepsin E 1
17482464 10.1016/j.bmcl.2007.04.052 Unchecked 1

Data from ChEMBL 36 via Core Engine