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Compound Detail

CHEMBL523189

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CC(=O)NCc1cc(-c2cc3nc(NC4CC4)c4ncn(C)c4n3n2)ccc1F

Basic Information

ChEMBL ID CHEMBL523189
Phase Preclinical
Structure Type MOL
InChI Key VBGRSDHDLOPNMH-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

393.4
MW (Da)
2.63
ALogP
7
HBA
2
HBD
89.1
PSA (Ų)
0.54
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 C20H20FN7O
MW 393.43
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.80

Activity Summary

IC50 5 meas. best 6.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 6.55 6.55 279.0 2
PBMC
CHEMBL613107
IC50 6.14 6.14 730.0 1
Inhibitor of nuclear factor kappa-B kinase subunit alpha
CHEMBL3476
IC50 5.01 5.01 9700.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19267461 10.1021/jm8015816 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
19267461 10.1021/jm8015816 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
21087862 10.1016/j.bmcl.2010.10.133 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
21087862 10.1016/j.bmcl.2010.10.133 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
21087862 10.1016/j.bmcl.2010.10.133 PBMC 1

Data from ChEMBL 36 via Core Engine