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Compound Detail

CHEMBL4452410

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Cc1ccc(C(=O)Nc2cccc3c(-c4nc(NC(=O)C5CC5)ncc4C)c[nH]c23)c(C)n1

Basic Information

ChEMBL ID CHEMBL4452410
Phase Preclinical
Structure Type MOL
InChI Key JOMKOBKADOLODH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

440.5
MW (Da)
4.55
ALogP
5
HBA
3
HBD
112.7
PSA (Ų)
0.42
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N6O2
MW 440.51
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.31

Activity Summary

IC50 2 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
IC50 7.37 7.37 43.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 5.6 5.6 2500.0 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