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Compound Detail

CHEMBL5418494

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CNCCCCCn1c(-c2ncc(-c3ccc4ccccc4c3)n2CCCC(C)(C)C)cnc1I

Basic Information

ChEMBL ID CHEMBL5418494
Phase Preclinical
Structure Type MOL
InChI Key PYVKCKXGZHKWHI-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

583.6
MW (Da)
7.39
ALogP
5
HBA
1
HBD
47.7
PSA (Ų)
0.15
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38IN5
MW 583.56
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.51

Activity Summary

IC50 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PCSK9/LDLR
CHEMBL4523996
IC50 8.15 8.15 7.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PCSK9/LDLR IC50 = 7.0 nM 8.15 Inhibition of His-tagged PCSK9 to recombinant LDLR (unknown origin) protein-prot... 37261954

Literature References

PubMed DOI Target Context # Activities
37261954 10.1021/acs.jmedchem.3c00279 Unchecked 4
37261954 10.1021/acs.jmedchem.3c00279 Proprotein convertase subtilisin/kexin type 9 2
37261954 10.1021/acs.jmedchem.3c00279 HepG2 1
37261954 10.1021/acs.jmedchem.3c00279 PCSK9/LDLR 1
37261954 10.1021/acs.jmedchem.3c00279 3-hydroxy-3-methylglutaryl-coenzyme A reductase 1

Data from ChEMBL 36 via Core Engine