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Compound Detail

CHEMBL4517253

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Cc1nc2c(c(-c3ccc4oc(N)nc4c3)nn2C(C)C)c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL4517253
Phase Preclinical
Structure Type MOL
InChI Key VYGVLHBRKJFFMR-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

324.3
MW (Da)
2.40
ALogP
7
HBA
2
HBD
115.6
PSA (Ų)
0.58
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 C16H16N6O2
MW 324.34
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.23

Activity Summary

IC50 2 meas. best 7.35
Ki 1 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase mTOR
CHEMBL2842
Ki 7.4 7.4 40.0 1
mTORC1
CHEMBL4296661
IC50 7.35 7.35 45.0 1
mTORC2
CHEMBL4523999
IC50 7.05 7.05 90.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31749911 10.1021/acsmedchemlett.9b00401 No relevant target 2
31749911 10.1021/acsmedchemlett.9b00401 ADMET 2
31749911 10.1021/acsmedchemlett.9b00401 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
31749911 10.1021/acsmedchemlett.9b00401 mTORC2 1
31749911 10.1021/acsmedchemlett.9b00401 mTORC1 1
31749911 10.1021/acsmedchemlett.9b00401 Serine/threonine-protein kinase mTOR 1

Data from ChEMBL 36 via Core Engine