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Compound Detail

CHEMBL398387

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CCc1nc(N)nc(N)c1-c1ccc2c(c1)N(CCNC(C)=O)C(=O)C1(CC1)O2

Basic Information

ChEMBL ID CHEMBL398387
Phase Preclinical
Structure Type MOL
InChI Key ULSULMMOPVCYQW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

396.4
MW (Da)
1.26
ALogP
7
HBA
3
HBD
136.5
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H24N6O3
MW 396.45
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.66

Activity Summary

IC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 7.0 7.0 100.0 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 = 100.0 nM 7.0 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 Caco-2 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 3A4 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

Data from ChEMBL 36 via Core Engine