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Compound Detail

CHEMBL374440

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COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(C#N)s3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL374440
Phase Preclinical
Structure Type MOL
InChI Key PYVMYBZZIWFCPE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

459.4
MW (Da)
5.57
ALogP
7
HBA
0
HBD
69.3
PSA (Ų)
0.38
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16F3N3O3S
MW 459.45
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 6.6 6.6 251.2 1
Serine/threonine-protein kinase PLK1
CHEMBL3024
IC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16997559 10.1016/j.bmcl.2006.09.018 Inhibitor of nuclear factor kappa-B kinase subunit epsilon 1
19097784 10.1016/j.bmcl.2008.11.041 Serine/threonine-protein kinase PLK1 1

Data from ChEMBL 36 via Core Engine