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Compound Detail

CHEMBL1092189

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COc1ccc2c(c1)c(/C=C1\Oc3cc(O)cc(O)c3C1=O)c(C)n2CCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL1092189
Phase Preclinical
Structure Type MOL
InChI Key FWAOTUPZXQMHPH-IWIPYMOSSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

464.5
MW (Da)
3.71
ALogP
8
HBA
2
HBD
93.4
PSA (Ų)
0.54
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28N2O6
MW 464.52
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.42

Activity Summary

IC50 6 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 8.1 8.1 8.0 1
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 7.75 7.75 18.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
IC50 7.12 7.12 76.0 1
PC-3
CHEMBL390
IC50 5.62 5.62 2400.0 1
LoVo
CHEMBL614721
IC50 5.34 5.34 4600.0 1
Caco-2
CHEMBL614058
IC50 5.33 5.33 4700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20303263 10.1016/j.bmcl.2010.02.082 Unchecked 2
20303263 10.1016/j.bmcl.2010.02.082 Serine/threonine-protein kinase mTOR 1
20303263 10.1016/j.bmcl.2010.02.082 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
20303263 10.1016/j.bmcl.2010.02.082 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
20303263 10.1016/j.bmcl.2010.02.082 No relevant target 1
20303263 10.1016/j.bmcl.2010.02.082 Caco-2 1
20303263 10.1016/j.bmcl.2010.02.082 LoVo 1
20303263 10.1016/j.bmcl.2010.02.082 PC-3 1
20303263 10.1016/j.bmcl.2010.02.082 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine