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Compound Detail

CHEMBL400431

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CCc1nc(N)nc(N)c1-c1ccc2c(c1)N(CCCOC)C(=O)C(C)(C)O2

Basic Information

ChEMBL ID CHEMBL400431
Phase Preclinical
Structure Type MOL
InChI Key WPAPODFGOZXFLG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
2.41
ALogP
7
HBA
2
HBD
116.6
PSA (Ų)
0.73
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C20H27N5O3
MW 385.47
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.73

Activity Summary

IC50 1 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 7.05 7.05 90.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.6667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Renin IC50 = 90.0 nM 7.05 Inhibition of human renin by fluorescent tGFP assay 17574423

Literature References

PubMed DOI Target Context # Activities
17574423 10.1016/j.bmc.2007.05.069 Renin 1
17574423 10.1016/j.bmc.2007.05.069 Liver microsomes 1
17574423 10.1016/j.bmc.2007.05.069 No relevant target 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 3A4 1
17574423 10.1016/j.bmc.2007.05.069 Caco-2 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 2D6 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 2C9 1
28601508 10.1016/j.bmc.2017.05.032 No relevant target 1

Data from ChEMBL 36 via Core Engine