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Compound Detail

CHEMBL3125723

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COc1ccc(-c2nc3c(NCCCNC(=O)C4CCCC4)c(C(N)=S)cnc3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL3125723
Phase Preclinical
Structure Type MOL
InChI Key UOFZOMWGIVJIKW-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

452.6
MW (Da)
3.38
ALogP
6
HBA
4
HBD
118.0
PSA (Ų)
0.29
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28N6O2S
MW 452.58
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.18

Activity Summary

IC50 4 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 7.34 7.06 46.0 2
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 6.35 6.35 448.0 1
Aurora kinase B
CHEMBL2185
IC50 6.05 6.05 889.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24462666 10.1016/j.bmcl.2013.12.123 Serine/threonine-protein kinase TBK1 2
24462666 10.1016/j.bmcl.2013.12.123 Cyclin-dependent kinase 2 1
24462666 10.1016/j.bmcl.2013.12.123 Aurora kinase B 1
24462666 10.1016/j.bmcl.2013.12.123 Inhibitor of nuclear factor kappa-B kinase subunit epsilon 1

Data from ChEMBL 36 via Core Engine