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Compound Detail

CHEMBL4528263

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CCN1CCC(Nc2cc(-c3ncnc4c3CN(c3cnc(OC)c(C)c3)CC4)ccn2)CC1

Basic Information

ChEMBL ID CHEMBL4528263
Phase Preclinical
Structure Type MOL
InChI Key YDIOYIKLGMGEOU-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

459.6
MW (Da)
3.71
ALogP
8
HBA
1
HBD
79.3
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N7O
MW 459.60
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.36

Activity Summary

IC50 3 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B-cell
CHEMBL614701
IC50 8.32 8.32 4.8 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
IC50 8.07 8.07 8.5 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 5.34 5.34 4600.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 160.0 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30755348 10.1016/j.bmc.2019.02.001 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
30755348 10.1016/j.bmc.2019.02.001 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
30755348 10.1016/j.bmc.2019.02.001 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
30755348 10.1016/j.bmc.2019.02.001 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
30755348 10.1016/j.bmc.2019.02.001 B-cell 1
30755348 10.1016/j.bmc.2019.02.001 ADMET 1

Data from ChEMBL 36 via Core Engine