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Compound Detail

CHEMBL2011940

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Nc1cccc(-c2nc3c(NCCCNC(=O)C4CCC4)c(Br)cnc3[nH]2)c1

Basic Information

ChEMBL ID CHEMBL2011940
Phase Preclinical
Structure Type MOL
InChI Key ZFQFDCSTGATGQP-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

443.4
MW (Da)
3.69
ALogP
5
HBA
4
HBD
108.7
PSA (Ų)
0.33
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 C20H23BrN6O
MW 443.35
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.21

Activity Summary

IC50 4 meas. best 8.52
EC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 8.52 8.52 3.0 1
Aurora kinase B
CHEMBL2185
IC50 8.4 8.4 4.0 1
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 8.4 8.4 4.0 1
Serine/threonine-protein kinase TBK1
CHEMBL5408
EC50 8.4 8.4 4.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.81 6.81 155.0 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