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Compound Detail

CHEMBL1807619

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O=C(NC[C@@H]1C[C@@H](F)CN1)c1ccc(-c2cnc3ccc(NC4CCCC4)nn23)cc1F

Basic Information

ChEMBL ID CHEMBL1807619
Phase Preclinical
Structure Type MOL
InChI Key WLKSMJZJHGIIIB-WBVHZDCISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

440.5
MW (Da)
3.32
ALogP
6
HBA
3
HBD
83.3
PSA (Ų)
0.55
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 C23H26F2N6O
MW 440.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.38

Activity Summary

IC50 2 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 7.8 7.8 16.0 1
Blood
CHEMBL613561
IC50 6.51 6.51 310.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21705219 10.1016/j.bmcl.2011.05.115 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
21705219 10.1016/j.bmcl.2011.05.115 Blood 1
21705219 10.1016/j.bmcl.2011.05.115 Plasma 1
21705219 10.1016/j.bmcl.2011.05.115 Liver 1
21705219 10.1016/j.bmcl.2011.05.115 Liver microsomes 1
21705219 10.1016/j.bmcl.2011.05.115 No relevant target 1
21705219 10.1016/j.bmcl.2011.05.115 ADMET 1
21705219 10.1016/j.bmcl.2011.05.115 Mus musculus 1

Data from ChEMBL 36 via Core Engine