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Compound Detail

CHEMBL563554

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CNc1nc2[nH]c(-c3cccc(CNC(=O)CN(C)C)c3)cc2c2c1ncn2C

Basic Information

ChEMBL ID CHEMBL563554
Phase Preclinical
Structure Type MOL
InChI Key KGIXECNIEFMEFX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

391.5
MW (Da)
2.34
ALogP
6
HBA
3
HBD
90.9
PSA (Ų)
0.47
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 C21H25N7O
MW 391.48
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.01

Activity Summary

IC50 2 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit alpha
CHEMBL3476
IC50 7.1 7.1 79.0 1
PBMC
CHEMBL613107
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19376699 10.1016/j.bmcl.2009.03.159 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
19376699 10.1016/j.bmcl.2009.03.159 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
19376699 10.1016/j.bmcl.2009.03.159 PBMC 1

Data from ChEMBL 36 via Core Engine