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Compound Detail

CHEMBL1090131

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COc1ccc2c(c1)c(/C=C1\Oc3cc(O)cc(O)c3C1=O)cn2CCN1CCN(CCCO)CC1

Basic Information

ChEMBL ID CHEMBL1090131
Phase Preclinical
Structure Type MOL
InChI Key LKJWRWGSGQGEJA-MXAYSNPKSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

493.6
MW (Da)
2.68
ALogP
9
HBA
3
HBD
107.6
PSA (Ų)
0.41
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N3O6
MW 493.56
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.36

Activity Summary

IC50 3 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 7.44 7.44 36.0 1
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 6.67 6.67 215.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
IC50 6.01 6.01 976.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20303263 10.1016/j.bmcl.2010.02.082 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

Data from ChEMBL 36 via Core Engine