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Compound Detail

CHEMBL3401981

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Oc1cc([C@H]2C3CCC(CC3)[C@@H]2Nc2nc(-c3c[nH]c4ncc(F)cc34)ncc2F)on1

Basic Information

ChEMBL ID CHEMBL3401981
Phase Preclinical
Structure Type MOL
InChI Key JYDWJFDOWRSYSW-DJZCKWSOSA-N
4
Targets
5
Activities
3
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

438.4
MW (Da)
4.38
ALogP
7
HBA
3
HBD
112.8
PSA (Ų)
0.43
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20F2N6O2
MW 438.44
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.64

Activity Summary

Ki 3 meas. best 6.16
EC50 1 meas. best 8.7
IC50 1 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Influenza A virus
CHEMBL613740
IC50 9.0 9.0 1.0 1
Influenza A virus
CHEMBL613740
EC50 8.7 8.7 2.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
Ki 6.16 6.16 690.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
Ki 5.89 5.89 1300.0 1
Glycogen synthase kinase-3
CHEMBL2095188
Ki 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25827523 10.1016/j.bmcl.2015.03.013 Influenza A virus 3
25827523 10.1016/j.bmcl.2015.03.013 Interleukin-1 receptor-associated kinase 4 1
25827523 10.1016/j.bmcl.2015.03.013 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
25827523 10.1016/j.bmcl.2015.03.013 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
25827523 10.1016/j.bmcl.2015.03.013 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
25827523 10.1016/j.bmcl.2015.03.013 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
25827523 10.1016/j.bmcl.2015.03.013 Hepatocyte growth factor receptor 1
25827523 10.1016/j.bmcl.2015.03.013 Serine/threonine-protein kinase PLK1 1
25827523 10.1016/j.bmcl.2015.03.013 Cyclin-dependent kinase 2 1
25827523 10.1016/j.bmcl.2015.03.013 Tyrosine-protein kinase SYK 1
25827523 10.1016/j.bmcl.2015.03.013 cAMP-dependent protein kinase catalytic subunit alpha 1
25827523 10.1016/j.bmcl.2015.03.013 Proto-oncogene tyrosine-protein kinase Src 1
25827523 10.1016/j.bmcl.2015.03.013 Vascular endothelial growth factor receptor 2 1
25827523 10.1016/j.bmcl.2015.03.013 Rho-associated protein kinase 1
25827523 10.1016/j.bmcl.2015.03.013 Mitogen-activated protein kinase 10 1
25827523 10.1016/j.bmcl.2015.03.013 Receptor-type tyrosine-protein kinase FLT3 1
25827523 10.1016/j.bmcl.2015.03.013 Glycogen synthase kinase-3 1
25827523 10.1016/j.bmcl.2015.03.013 Tyrosine-protein kinase JAK2 1

Data from ChEMBL 36 via Core Engine