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Compound Detail

CHEMBL4439287

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Cc1ccc(-n2ccc3c(Nc4cccc(NC(=O)c5ccc(NC(=O)/C=C/CN(C)C)cc5)c4)ncnc32)cc1

Basic Information

ChEMBL ID CHEMBL4439287
Phase Preclinical
Structure Type MOL
InChI Key QSHQSGKUSRNJPU-VMPITWQZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

545.6
MW (Da)
5.78
ALogP
7
HBA
3
HBD
104.2
PSA (Ų)
0.20
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H31N7O2
MW 545.65
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -1.29

Activity Summary

IC50 2 meas. best 5.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha
CHEMBL1795194
IC50 5.87 5.87 1340.0 1
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta
CHEMBL5667
IC50 5.0 5.0 9900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32184968 10.1021/acsmedchemlett.9b00402 Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha 2
32184968 10.1021/acsmedchemlett.9b00402 Phosphatidylinositol 5-phosphate 4-kinase type-2 beta 2
32184968 10.1021/acsmedchemlett.9b00402 Ribosomal protein S6 kinase alpha-4 1
32184968 10.1021/acsmedchemlett.9b00402 Non-receptor tyrosine-protein kinase TYK2 1
32184968 10.1021/acsmedchemlett.9b00402 Casein kinase II subunit alpha' 1
32184968 10.1021/acsmedchemlett.9b00402 Platelet-derived growth factor receptor beta 1
32184968 10.1021/acsmedchemlett.9b00402 1-phosphatidylinositol 3-phosphate 5-kinase 1
35148092 10.1021/acs.jmedchem.1c01819 Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma 1

Data from ChEMBL 36 via Core Engine