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Compound Detail

CHEMBL179242

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O=c1cc(N2CCOCC2)nc2c3ccccc3ccn12

Basic Information

ChEMBL ID CHEMBL179242
Phase Preclinical
Structure Type MOL
InChI Key BVRDQVRQVGRNHG-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

281.3
MW (Da)
1.68
ALogP
5
HBA
0
HBD
46.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15N3O2
MW 281.31
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.58

Activity Summary

IC50 5 meas. best 6.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA-dependent protein kinase catalytic subunit
CHEMBL3142
IC50 6.55 6.55 280.0 2
Unchecked
CHEMBL612545
IC50 6.55 6.55 280.0 1
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 5.28 5.28 5300.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17562705 10.1074/jbc.m704741200 Serine/threonine-protein kinase mTOR 7
17562705 10.1074/jbc.m704741200 Unchecked 3
17562705 10.1074/jbc.m704741200 NON-PROTEIN TARGET 3
17562705 10.1074/jbc.m704741200 Ribosomal protein S6 kinase beta-1 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
17562705 10.1074/jbc.m704741200 Fibroblast 2
17562705 10.1074/jbc.m704741200 RAC-alpha serine/threonine-protein kinase 2
- 10.6019/CHEMBL3301361 No relevant target 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
17562705 10.1074/jbc.m704741200 Tyrosine-protein kinase BTK 1
17562705 10.1074/jbc.m704741200 Glycogen synthase kinase-3 beta 1
17562705 10.1074/jbc.m704741200 Receptor-type tyrosine-protein kinase FLT3 1
17562705 10.1074/jbc.m704741200 Casein kinase II subunit alpha 1
17562705 10.1074/jbc.m704741200 Casein kinase I isoform gamma-2 1
17562705 10.1074/jbc.m704741200 Serine/threonine-protein kinase Chk1 1
17562705 10.1074/jbc.m704741200 Cyclin-dependent kinase 1/cyclin B1 1
17562705 10.1074/jbc.m704741200 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
15658870 10.1021/jm049526a Serine/threonine-protein kinase mTOR 1
15658870 10.1021/jm049526a Serine/threonine-protein kinase ATR 1
15658870 10.1021/jm049526a Serine-protein kinase ATM 1

Data from ChEMBL 36 via Core Engine