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Compound Detail

CHEMBL182407

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N#Cc1c(C2CCCNC2)cc(-c2c(O)cccc2OCC2CC2)nc1N

Basic Information

ChEMBL ID CHEMBL182407
Phase Preclinical
Structure Type MOL
InChI Key LRAIEGOIIAZHRP-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

364.4
MW (Da)
3.16
ALogP
6
HBA
3
HBD
104.2
PSA (Ų)
0.75
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 C21H24N4O2
MW 364.45
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.44

Activity Summary

IC50 4 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 8.52 8.52 3.0 3
A549
CHEMBL392
IC50 7.1 7.1 80.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15225718 10.1016/j.bmcl.2004.05.041 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
15225718 10.1016/j.bmcl.2004.05.041 A549 1
21708416 10.1016/j.ejmech.2011.05.066 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
23501112 10.1016/j.ejmech.2013.01.045 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine