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Compound Detail

CHEMBL4239569

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COc1ccc(-c2ccc3c(N4CCOCC4)nc(C#N)nc3n2)cc1CO

Basic Information

ChEMBL ID CHEMBL4239569
Phase Preclinical
Structure Type MOL
InChI Key YORDELGQXBGIHM-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

377.4
MW (Da)
1.90
ALogP
8
HBA
1
HBD
104.4
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19N5O3
MW 377.40
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.97

Activity Summary

IC50 4 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 7.5 7.5 32.0 1
SK-OV-3
CHEMBL614925
IC50 6.18 6.18 660.0 1
U-87 MG
CHEMBL614247
IC50 6.04 6.04 920.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29945756 10.1016/j.bmc.2018.06.025 Serine/threonine-protein kinase mTOR 1
29945756 10.1016/j.bmc.2018.06.025 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
29945756 10.1016/j.bmc.2018.06.025 U-87 MG 1
29945756 10.1016/j.bmc.2018.06.025 MCF7 1
29945756 10.1016/j.bmc.2018.06.025 PC-3 1
29945756 10.1016/j.bmc.2018.06.025 SK-OV-3 1

Data from ChEMBL 36 via Core Engine