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Compound Detail

CHEMBL4566849

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C=CC(=O)Nc1ccc(CNc2cc(Nc3ccc(N4CCOCC4)cc3)ncn2)cc1

Basic Information

ChEMBL ID CHEMBL4566849
Phase Preclinical
Structure Type MOL
InChI Key ZPJZUNKZSHRLML-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
3.79
ALogP
7
HBA
3
HBD
91.4
PSA (Ų)
0.47
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26N6O2
MW 430.51
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.34

Activity Summary

IC50 3 meas. best 8.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 8.08 8.08 8.4 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 6.04 6.04 916.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 5.94 5.94 1159.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30853331 10.1016/j.bmc.2019.03.009 Unchecked 2
30853331 10.1016/j.bmc.2019.03.009 Tyrosine-protein kinase JAK3 1
30853331 10.1016/j.bmc.2019.03.009 Tyrosine-protein kinase JAK2 1
30853331 10.1016/j.bmc.2019.03.009 Tyrosine-protein kinase JAK1 1
30853331 10.1016/j.bmc.2019.03.009 Non-receptor tyrosine-protein kinase TYK2 1

Data from ChEMBL 36 via Core Engine