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Compound Detail

CHEMBL4637818

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Cc1ccc(C(=O)Nc2cc(N3CCN(C)CC3)cc(-n3cnc(C)c3)c2)cc1

Basic Information

ChEMBL ID CHEMBL4637818
Phase Preclinical
Structure Type MOL
InChI Key GFKHNUHEUMXRLU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

389.5
MW (Da)
3.49
ALogP
5
HBA
1
HBD
53.4
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N5O
MW 389.50
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 4.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PCSK9/LDLR
CHEMBL4523996
IC50 4.58 4.58 26300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PCSK9/LDLR IC50 = 26300.0 nM 4.58 Inhibition of recombinant human His-tagged PCSK9 interaction with recombinant LD... 32051094

Literature References

PubMed DOI Target Context # Activities
32051094 10.1016/j.bmc.2020.115344 PCSK9/LDLR 1
32051094 10.1016/j.bmc.2020.115344 Mast/stem cell growth factor receptor Kit 1
32051094 10.1016/j.bmc.2020.115344 Tyrosine-protein kinase ABL1 1
32051094 10.1016/j.bmc.2020.115344 Platelet-derived growth factor receptor beta 1
32051094 10.1016/j.bmc.2020.115344 Proto-oncogene tyrosine-protein kinase Src 1

Data from ChEMBL 36 via Core Engine