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Compound Detail

CHEMBL5639918

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CNCCNC(=O)c1ccc(NC(=O)Nc2ccc(-c3nc(OC)nc(N4CCOCC4)n3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL5639918
Phase Preclinical
Structure Type MOL
InChI Key RHRDCLZTHCOWGQ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
1.98
ALogP
9
HBA
4
HBD
142.6
PSA (Ų)
0.32
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30N8O4
MW 506.57
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.38

Activity Summary

IC50 5 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 8.62 8.62 2.4 1
JeKo-1
CHEMBL4296445
IC50 5.96 5.96 1100.0 1
HL-60
CHEMBL383
IC50 5.51 5.51 3100.0 1
MM1.S
CHEMBL4296471
IC50 5.48 5.48 3300.0 1
MDA-MB-231
CHEMBL400
IC50 5.38 5.38 4200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37948955 10.1016/j.ejmech.2023.115915 JeKo-1 30
37948955 10.1016/j.ejmech.2023.115915 Unchecked 2
37948955 10.1016/j.ejmech.2023.115915 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
37948955 10.1016/j.ejmech.2023.115915 Histone deacetylase 1 1
37948955 10.1016/j.ejmech.2023.115915 Histone deacetylase 2 1
37948955 10.1016/j.ejmech.2023.115915 Histone deacetylase 3 1
37948955 10.1016/j.ejmech.2023.115915 MM1.S 1
37948955 10.1016/j.ejmech.2023.115915 HL-60 1
37948955 10.1016/j.ejmech.2023.115915 MDA-MB-231 1
37948955 10.1016/j.ejmech.2023.115915 L02 1
37948955 10.1016/j.ejmech.2023.115915 Molecular identity unknown 1

Data from ChEMBL 36 via Core Engine