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Compound Detail

CHEMBL384117

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CC(C)c1nnc2ccc(-c3ocnc3-c3cccc(F)c3)cn12

Basic Information

ChEMBL ID CHEMBL384117
Phase Preclinical
Structure Type MOL
InChI Key PPPKNNQINQHKNZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

322.3
MW (Da)
4.31
ALogP
5
HBA
0
HBD
56.2
PSA (Ų)
0.56
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H15FN4O
MW 322.34
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.73

Activity Summary

IC50 2 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.42 7.42 37.8 1
Monocyte
CHEMBL614076
IC50 6.87 6.87 135.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 37.8 nM 7.42 Inhibition of p38alpha 16759861
Monocyte IC50 = 135.0 nM 6.87 Inhibition of LPS-induced TNFalpha production in human monocytes 16759861

Literature References

PubMed DOI Target Context # Activities
16759861 10.1016/j.bmcl.2006.05.056 Hepatocyte 1
16759861 10.1016/j.bmcl.2006.05.056 Monocyte 1
16759861 10.1016/j.bmcl.2006.05.056 Homo sapiens 1
16759861 10.1016/j.bmcl.2006.05.056 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine