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Compound Detail

CHEMBL1288160

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O=C(Cc1cccc2cnccc12)Nc1scnc1-c1cscn1

Basic Information

ChEMBL ID CHEMBL1288160
Phase Preclinical
Structure Type MOL
InChI Key BGGSTZPBQKGLOJ-UHFFFAOYSA-N
3
Targets
7
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
4.00
ALogP
6
HBA
1
HBD
67.8
PSA (Ų)
0.60
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 C17H12N4OS2
MW 352.44
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.77

Activity Summary

IC50 7 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 7.32 7.32 48.0 2
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.11 7.11 77.0 2
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 6.33 5.9867 470.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21071223 10.1016/j.bmcl.2010.10.066 Mitogen-activated protein kinase 10 2
21071223 10.1016/j.bmcl.2010.10.066 Mitogen-activated protein kinase 1 2
21071223 10.1016/j.bmcl.2010.10.066 Dual specificity tyrosine-phosphorylation-regulated kinase 1B 1
35200035 10.1021/acs.jmedchem.1c01947 Mitogen-activated protein kinase 9 1
21071223 10.1016/j.bmcl.2010.10.066 Serine/threonine-protein kinase PAK 4 1
21071223 10.1016/j.bmcl.2010.10.066 Serine/threonine-protein kinase MARK2 1
21071223 10.1016/j.bmcl.2010.10.066 Tyrosine-protein kinase Lck 1
21071223 10.1016/j.bmcl.2010.10.066 Tyrosine-protein kinase JAK1 1
21071223 10.1016/j.bmcl.2010.10.066 Insulin receptor 1
21071223 10.1016/j.bmcl.2010.10.066 Glycogen synthase kinase-3 beta 1
21071223 10.1016/j.bmcl.2010.10.066 Receptor-type tyrosine-protein kinase FLT3 1
21071223 10.1016/j.bmcl.2010.10.066 Receptor tyrosine-protein kinase erbB-4 1
21071223 10.1016/j.bmcl.2010.10.066 Mitogen-activated protein kinase 8 1
21071223 10.1016/j.bmcl.2010.10.066 Macrophage colony-stimulating factor 1 receptor 1
21071223 10.1016/j.bmcl.2010.10.066 Cyclin-dependent kinase 5/CDK5 activator 1 1
21071223 10.1016/j.bmcl.2010.10.066 Cyclin-dependent kinase 2/cyclin A 1
21071223 10.1016/j.bmcl.2010.10.066 Cyclin-dependent kinase 1/cyclin B 1
21071223 10.1016/j.bmcl.2010.10.066 Calcium/calmodulin-dependent protein kinase type II subunit alpha 1
21071223 10.1016/j.bmcl.2010.10.066 RAC-alpha serine/threonine-protein kinase 1
21071223 10.1016/j.bmcl.2010.10.066 Tyrosine-protein kinase ABL1 1

Data from ChEMBL 36 via Core Engine