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Compound Detail

CHEMBL173484

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N#Cc1c(-c2cccc(NC(=O)CCN3CCCCC3)c2)cc(-c2ccccc2O)nc1N

Basic Information

ChEMBL ID CHEMBL173484
Phase Preclinical
Structure Type MOL
InChI Key OGKJHWSTJKFLOO-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

441.5
MW (Da)
4.39
ALogP
6
HBA
3
HBD
115.3
PSA (Ų)
0.52
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N5O2
MW 441.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.47

Activity Summary

IC50 5 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 6.22 6.22 600.0 2
A549
CHEMBL392
IC50 5.16 5.16 7000.0 2
Inhibitor of nuclear factor kappa-B kinase subunit alpha
CHEMBL3476
IC50 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12617920 10.1016/s0960-894x(02)01046-6 Mus musculus 2
12617920 10.1016/s0960-894x(02)01046-6 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
12617920 10.1016/s0960-894x(02)01046-6 A549 1
12617920 10.1016/s0960-894x(02)01046-6 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
12617920 10.1016/s0960-894x(02)01046-6 Tyrosine-protein kinase SYK 1
12617920 10.1016/s0960-894x(02)01046-6 Dual specificity mitogen-activated protein kinase kinase 4 1
15225717 10.1016/j.bmcl.2004.05.040 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
15225717 10.1016/j.bmcl.2004.05.040 A549 1

Data from ChEMBL 36 via Core Engine