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Compound Detail

CHEMBL3125725

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COc1ccc(-c2nc3c(OCCCNC(=O)C4CCCC4)c(Br)cnc3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL3125725
Phase Preclinical
Structure Type MOL
InChI Key WTQDVZNJLFUQDW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

473.4
MW (Da)
4.47
ALogP
5
HBA
2
HBD
89.1
PSA (Ų)
0.47
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25BrN4O3
MW 473.37
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.98

Activity Summary

IC50 2 meas. best 6.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
IC50 6.81 6.81 156.0 1
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 6.12 6.12 759.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine