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Compound Detail

CHEMBL5177612

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Nc1ncc(-c2cc(N3CCOC3=O)nc(N3CCOCC3)n2)c(C(F)(F)F)n1

Basic Information

ChEMBL ID CHEMBL5177612
Phase Preclinical
Structure Type MOL
InChI Key TZFXOFYWNLCGEL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

411.3
MW (Da)
1.33
ALogP
9
HBA
1
HBD
119.6
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16F3N7O3
MW 411.34
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.71

Activity Summary

IC50 3 meas. best 6.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.86 6.86 137.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
CHEMBL3608198
IC50 6.74 6.74 184.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL5169092
IC50 6.59 6.59 256.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35500094 10.1021/acs.jmedchem.2c00267 Serine/threonine-protein kinase mTOR 1
35500094 10.1021/acs.jmedchem.2c00267 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
35500094 10.1021/acs.jmedchem.2c00267 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
35500094 10.1021/acs.jmedchem.2c00267 Unchecked 1

Data from ChEMBL 36 via Core Engine