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Compound Detail

CHEMBL564099

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CNC(=O)Nc1ccc(-c2nc(N3CCOCC3)c3cnn(C4CCN(C)CC4)c3n2)cc1

Basic Information

ChEMBL ID CHEMBL564099
Phase Preclinical
Structure Type MOL
InChI Key GFDHDIYLLBVZPF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

450.6
MW (Da)
2.35
ALogP
8
HBA
2
HBD
100.4
PSA (Ų)
0.63
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H30N8O2
MW 450.55
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -2.03

Activity Summary

IC50 3 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 7.66 7.66 22.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 6.68 6.68 211.0 1
LNCaP
CHEMBL612518
IC50 6.13 6.13 733.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.03333 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19645448 10.1021/jm900851f Serine/threonine-protein kinase mTOR 1
19645448 10.1021/jm900851f Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
19645448 10.1021/jm900851f Unchecked 1
19645448 10.1021/jm900851f LNCaP 1
19645448 10.1021/jm900851f ADMET 1

Data from ChEMBL 36 via Core Engine