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Compound Detail

CHEMBL4251185

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COc1ccc(-c2ccc3c(N4CCOC[C@@H]4C)nc(C4CCOCC4)nc3n2)cc1CO

Basic Information

ChEMBL ID CHEMBL4251185
Phase Preclinical
Structure Type MOL
InChI Key SSTJSROOZICEBQ-INIZCTEOSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

450.5
MW (Da)
3.31
ALogP
8
HBA
1
HBD
89.8
PSA (Ų)
0.63
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 C25H30N4O4
MW 450.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.58

Activity Summary

IC50 5 meas. best 7.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 7.28 7.28 53.0 1
U-87 MG
CHEMBL614247
IC50 7.03 7.03 94.2 1
SK-OV-3
CHEMBL614925
IC50 6.93 6.93 118.5 1
MCF7
CHEMBL387
IC50 6.35 6.35 443.0 1
PC-3
CHEMBL390
IC50 6.32 6.32 476.0 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