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Compound Detail

CHEMBL3354192

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COC1CCN(c2nccc(Nc3cc4c(C(C)C)n[nH]c4cn3)n2)CC1

Basic Information

ChEMBL ID CHEMBL3354192
Phase Preclinical
Structure Type MOL
InChI Key GKMHWPHQBQHBKR-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

367.5
MW (Da)
3.23
ALogP
7
HBA
2
HBD
91.8
PSA (Ų)
0.72
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 -1.25

Activity Summary

Ki 3 meas. best 7.75
IC50 2 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
Ki 7.75 7.1133 18.0 3
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.32 6.32 476.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.65 5.65 2240.0 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 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

Data from ChEMBL 36 via Core Engine