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Compound Detail

CHEMBL4868065

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FC(F)(F)c1cncc(-c2ccc3ncc4nnc(C5CCOCC5)n4c3c2)c1

Basic Information

ChEMBL ID CHEMBL4868065
Phase Preclinical
Structure Type MOL
InChI Key WROQPSKLDRGJBM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
4.25
ALogP
6
HBA
0
HBD
65.2
PSA (Ų)
0.50
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16F3N5O
MW 399.38
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.46

Activity Summary

IC50 2 meas. best 5.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA-dependent protein kinase catalytic subunit
CHEMBL3142
IC50 5.91 5.91 1220.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform
CHEMBL3145
IC50 5.29 5.29 5080.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34428039 10.1021/acs.jmedchem.1c00762 DNA-dependent protein kinase catalytic subunit 1
34428039 10.1021/acs.jmedchem.1c00762 ATR/ATRIP 1
34428039 10.1021/acs.jmedchem.1c00762 Serine-protein kinase ATM 1
34428039 10.1021/acs.jmedchem.1c00762 Serine/threonine-protein kinase mTOR 1
34428039 10.1021/acs.jmedchem.1c00762 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1

Data from ChEMBL 36 via Core Engine