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Compound Detail

CHEMBL3354566

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Cn1c(=O)n(-c2ccc(C3(C#N)CC3)cc2)c2c3cc(-c4cnc5ccccc5c4)ccc3ncc21

Basic Information

ChEMBL ID CHEMBL3354566
Phase Preclinical
Structure Type MOL
InChI Key MPZUHFMONDTNMH-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
5.65
ALogP
6
HBA
0
HBD
76.5
PSA (Ų)
0.34
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H21N5O
MW 467.53
Aromatic Rings 6
Heavy Atoms 36
NP-Likeness -0.87

Activity Summary

IC50 5 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 8.7 8.7 2.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 8.15 8.15 7.0 1
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha
CHEMBL1075102
IC50 7.47 7.47 34.0 1
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta
CHEMBL5554
IC50 7.36 7.36 44.0 1
Unchecked
CHEMBL612545
IC50 6.35 6.35 450.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25589915 10.1021/ml500354e Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta 1
25589915 10.1021/ml500354e Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha 1
25589915 10.1021/ml500354e Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma 1
25589915 10.1021/ml500354e Unchecked 1
25589915 10.1021/ml500354e Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
25589915 10.1021/ml500354e Serine/threonine-protein kinase mTOR 1

Data from ChEMBL 36 via Core Engine