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Compound Detail

CHEMBL444636

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CC(C)Cn1c(N)nc2ccc(-c3[nH]c(-c4c(F)cccc4F)nc3-c3ccccc3)cc21.CS(=O)(=O)O

Basic Information

ChEMBL ID CHEMBL444636
Phase Preclinical
Structure Type MOL
InChI Key NADJHSGVCGEDEE-UHFFFAOYSA-N
Parent Compound CHEMBL1185992
Active Moiety CHEMBL1185992
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
6.28
ALogP
4
HBA
2
HBD
72.5
PSA (Ų)
0.34
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27F2N5O3S
MW 539.61
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -1.07

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 8.0 8.0 9.9 1
Macrophage
CHEMBL612578
IC50 7.32 7.32 47.5 1
Mitogen-activated protein kinase 14
CHEMBL2336
IC50 7.11 7.11 78.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18039577 10.1016/j.bmcl.2007.10.106 Mitogen-activated protein kinase 14 2
18039577 10.1016/j.bmcl.2007.10.106 Macrophage 1

Data from ChEMBL 36 via Core Engine