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Compound Detail

CHEMBL2011930

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

Basic Information

ChEMBL ID CHEMBL2011930
Phase Preclinical
Structure Type MOL
InChI Key CZBLMYRJPRLVRE-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

460.4
MW (Da)
4.36
ALogP
5
HBA
3
HBD
91.9
PSA (Ų)
0.46
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 C21H26BrN5O2
MW 460.38
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.03

Activity Summary

IC50 3 meas. best 8.15
EC50 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 8.15 8.15 7.0 1
Serine/threonine-protein kinase TBK1
CHEMBL5408
EC50 7.96 7.96 11.0 1
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 7.22 7.22 60.0 1
Aurora kinase B
CHEMBL2185
IC50 7.09 7.09 81.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22305584 10.1016/j.bmcl.2012.01.018 Serine/threonine-protein kinase TBK1 2
22305584 10.1016/j.bmcl.2012.01.018 Inhibitor of nuclear factor kappa-B kinase subunit epsilon 1
22305584 10.1016/j.bmcl.2012.01.018 Aurora kinase B 1
22305584 10.1016/j.bmcl.2012.01.018 Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine