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Compound Detail

CHEMBL3589322

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COc1cccc(-c2nc(N3CCOCC3)c3c(n2)N(c2ccccc2)C(=S)N2CCCC32)c1

Basic Information

ChEMBL ID CHEMBL3589322
Phase Preclinical
Structure Type MOL
InChI Key UUBFQGVOWRHYTF-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

473.6
MW (Da)
4.56
ALogP
6
HBA
0
HBD
54.0
PSA (Ų)
0.51
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 C26H27N5O2S
MW 473.60
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.21

Activity Summary

IC50 7 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL2498
IC50 6.16 6.16 695.0 1
HeLa
CHEMBL399
IC50 5.71 5.71 1970.0 1
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
CHEMBL5554
IC50 4.84 4.84 14560.0 1
SK-OV-3
CHEMBL614925
IC50 4.22 4.22 60460.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
IC50 4.15 4.15 71350.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26037808 10.1016/j.ejmech.2015.05.036 Unchecked 4
26037808 10.1016/j.ejmech.2015.05.036 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
26037808 10.1016/j.ejmech.2015.05.036 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
26037808 10.1016/j.ejmech.2015.05.036 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
26037808 10.1016/j.ejmech.2015.05.036 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
26037808 10.1016/j.ejmech.2015.05.036 Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta 1
26037808 10.1016/j.ejmech.2015.05.036 HeLa 1
26037808 10.1016/j.ejmech.2015.05.036 SK-OV-3 1

Data from ChEMBL 36 via Core Engine