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Compound Detail

CHEMBL426183

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COCCn1c(SC)nc(-c2ccc(F)cc2)c1-c1ccnc(NC(C)=O)c1

Basic Information

ChEMBL ID CHEMBL426183
Phase Preclinical
Structure Type MOL
InChI Key VNWXBCDASDHBCA-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

400.5
MW (Da)
4.08
ALogP
6
HBA
1
HBD
69.0
PSA (Ų)
0.61
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H21FN4O2S
MW 400.48
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.70

Activity Summary

IC50 6 meas. best 6.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.97 6.8633 108.0 3
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 6.7 6.7 202.0 1
Blood
CHEMBL613416
IC50 4.52 4.505 30500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15566301 10.1021/jm0496584 Blood 2
15566301 10.1021/jm0496584 Mitogen-activated protein kinase 14 1
15566301 10.1021/jm0496584 Cytochrome P450 1A2 1
15566301 10.1021/jm0496584 Cytochrome P450 2C9 1
15566301 10.1021/jm0496584 Cytochrome P450 2C19 1
15566301 10.1021/jm0496584 Cytochrome P450 2D6 1
15566301 10.1021/jm0496584 Cytochrome P450 3A4 1
20934337 10.1016/j.bmcl.2010.09.012 Mitogen-activated protein kinase 14 1
36490325 10.1021/acs.jmedchem.2c00799 Mitogen-activated protein kinase 14 1
36490325 10.1021/acs.jmedchem.2c00799 Mitogen-activated protein kinase 10 1

Data from ChEMBL 36 via Core Engine