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Compound Detail

CHEMBL4441479

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COc1nn(C)cc1Nc1ncc(C)c(-c2c[nH]c3c(NC(=O)c4cccnc4C)cccc23)n1

Basic Information

ChEMBL ID CHEMBL4441479
Phase Preclinical
Structure Type MOL
InChI Key VVOKUJIAOSWPTI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

468.5
MW (Da)
4.37
ALogP
8
HBA
3
HBD
122.6
PSA (Ų)
0.34
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N8O2
MW 468.52
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.41

Activity Summary

IC50 2 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 7.75 7.75 18.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32297743 10.1021/acs.jmedchem.9b01392 Tyrosine-protein kinase JAK1 1
32297743 10.1021/acs.jmedchem.9b01392 Tyrosine-protein kinase JAK2 1
32297743 10.1021/acs.jmedchem.9b01392 Unchecked 1
32297743 10.1021/acs.jmedchem.9b01392 No relevant target 1

Data from ChEMBL 36 via Core Engine