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Compound Detail

CHEMBL3354190

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COC1CCN(c2nccc(Nc3cc4c(cn3)ncn4C(C)C)n2)CC1

Basic Information

ChEMBL ID CHEMBL3354190
Phase Preclinical
Structure Type MOL
InChI Key GUKYWSVRGDINLN-UHFFFAOYSA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

367.5
MW (Da)
3.16
ALogP
8
HBA
1
HBD
81.0
PSA (Ų)
0.74
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H25N7O
MW 367.46
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.28

Activity Summary

Ki 4 meas. best 7.4
IC50 1 meas. best 5.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 7.4 6.9325 40.0 4
Cyclin-dependent kinase 2
CHEMBL301
IC50 5.65 5.65 2220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25383627 10.1021/jm501578n Epidermal growth factor receptor 3
25383627 10.1021/jm501578n Non-receptor tyrosine-protein kinase TYK2 3
25383627 10.1021/jm501578n Unchecked 2
25383627 10.1021/jm501578n No relevant target 2
25383627 10.1021/jm501578n Aurora kinase B 1
25383627 10.1021/jm501578n Vascular endothelial growth factor receptor 2 1
25383627 10.1021/jm501578n Cyclin-dependent kinase 2 1
25383627 10.1021/jm501578n Tyrosine-protein kinase JAK2 1
25383627 10.1021/jm501578n Mitogen-activated protein kinase kinase kinase kinase 4 1
25383627 10.1021/jm501578n Misshapen-like kinase 1 1
25383627 10.1021/jm501578n Maternal embryonic leucine zipper kinase 1
25383627 10.1021/jm501578n Serine/threonine-protein kinase 4 1
25383627 10.1021/jm501578n Tyrosine-protein kinase receptor TYRO3 1
25383627 10.1021/jm501578n Dual specificity protein kinase TTK 1
26455919 10.1021/acs.jmedchem.5b01412 Epidermal growth factor receptor 1
26455919 10.1021/acs.jmedchem.5b01412 No relevant target 1

Data from ChEMBL 36 via Core Engine