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Compound Detail

CHEMBL2011926

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COc1ccc(-c2nc3c(NCC4CCNCC4)c(Br)cnc3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL2011926
Phase Preclinical
Structure Type MOL
InChI Key WOTWXKACTZFRQE-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

416.3
MW (Da)
3.81
ALogP
5
HBA
3
HBD
74.9
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22BrN5O
MW 416.32
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.66

Activity Summary

IC50 4 meas. best 7.37
EC50 1 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
IC50 7.37 7.37 43.0 1
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 7.24 7.24 57.0 1
Serine/threonine-protein kinase TBK1
CHEMBL5408
EC50 6.96 6.96 111.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.87 6.87 135.0 1
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 6.58 6.58 265.0 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
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine