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Compound Detail

CHEMBL4552985

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C/C=C/C(=O)Nc1cccc(CNc2cc(Nc3cnn(C)c3)ncn2)c1

Basic Information

ChEMBL ID CHEMBL4552985
Phase Preclinical
Structure Type MOL
InChI Key GXAMADMEMDRBID-HWKANZROSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
3.08
ALogP
7
HBA
3
HBD
96.8
PSA (Ų)
0.56
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H21N7O
MW 363.43
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.64

Activity Summary

IC50 2 meas. best 6.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 6.47 6.47 342.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 5.88 5.88 1319.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine