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Compound Detail

CHEMBL4469876

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COc1ncc(C2=CCOCC2)cc1NS(=O)(=O)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4469876
Phase Preclinical
Structure Type MOL
InChI Key OZEVUWLUKNYTLV-UHFFFAOYSA-N
7
Targets
9
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
2.69
ALogP
5
HBA
1
HBD
77.5
PSA (Ų)
0.90
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H18N2O4S
MW 346.41
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.04

Activity Summary

IC50 9 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PI3-kinase p110-delta/p85-alpha
CHEMBL2111432
IC50 7.4 7.4 39.8 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
IC50 7.4 6.45 39.8 2
PI3K p110 beta/p85 alpha
CHEMBL3038510
IC50 6.4 6.4 398.1 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
CHEMBL3145
IC50 6.4 6.4 398.1 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
IC50 5.9 5.9 1258.9 2
PI3-kinase p110-alpha/p85-alpha
CHEMBL2111367
IC50 5.7 5.7 1995.3 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 5.7 5.7 1995.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 39.81 nM 7.4 Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated fo... 30532965
PI3-kinase p110-delta/p85-alpha IC50 = 39.81 nM 7.4 Inhibition of recombinant human N-terminal His6-tagged full length P110delta/ful... 34510892
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform IC50 = 398.11 nM 6.4 Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for... 30532965
PI3K p110 beta/p85 alpha IC50 = 398.11 nM 6.4 Inhibition of recombinant human N-terminal His6-tagged full length P110beta/full... 34510892
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 1258.93 nM 5.9 Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated fo... 30532965
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 1258.93 nM 5.9 Inhibition of recombinant human N-terminal His6-tagged full length P120gamma exp... 34510892
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform IC50 = 1995.26 nM 5.7 Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated fo... 30532965
PI3-kinase p110-alpha/p85-alpha IC50 = 1995.26 nM 5.7 Inhibition of recombinant human N-terminal His6-tagged full length P110alpha/ful... 34510892
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 3162.28 nM 5.5 Inhibition of PI3Kdelta in human whole blood assessed as reduction in cytostim-s... 34510892

Literature References

PubMed DOI Target Context # Activities
30532965 10.1021/acs.jmedchem.8b01556 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
30532965 10.1021/acs.jmedchem.8b01556 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
30532965 10.1021/acs.jmedchem.8b01556 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
30532965 10.1021/acs.jmedchem.8b01556 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
34510892 10.1021/acs.jmedchem.1c01102 PI3-kinase p110-delta/p85-alpha 1
34510892 10.1021/acs.jmedchem.1c01102 PI3-kinase p110-alpha/p85-alpha 1
34510892 10.1021/acs.jmedchem.1c01102 PI3K p110 beta/p85 alpha 1
34510892 10.1021/acs.jmedchem.1c01102 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
34510892 10.1021/acs.jmedchem.1c01102 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1

Data from ChEMBL 36 via Core Engine