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Compound Detail

CHEMBL3314277

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O=c1cc(-c2[nH]c(-c3ccc(-c4cn(CCO)nn4)cc3)nc2-c2ccc(F)cc2)cc[nH]1

Basic Information

ChEMBL ID CHEMBL3314277
Phase Preclinical
Structure Type MOL
InChI Key HJPSQYDUHYYPLU-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

442.4
MW (Da)
3.49
ALogP
6
HBA
3
HBD
112.5
PSA (Ų)
0.37
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H19FN6O2
MW 442.45
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -1.26

Activity Summary

IC50 4 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 6.3 6.3 500.0 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 4.97 4.97 10600.0 1
Casein kinase I isoform delta
CHEMBL2828
IC50 4.75 4.75 17900.0 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 4.73 4.73 18600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24930833 10.1016/j.bmcl.2014.05.080 Mitogen-activated protein kinase 14 1
24930833 10.1016/j.bmcl.2014.05.080 Casein kinase I isoform delta 1
24930833 10.1016/j.bmcl.2014.05.080 Tyrosine-protein kinase JAK1 1
24930833 10.1016/j.bmcl.2014.05.080 Tyrosine-protein kinase JAK2 1
24930833 10.1016/j.bmcl.2014.05.080 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine