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Compound Detail

CHEMBL219711

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COc1cc2ncn(-c3cc(OCc4ccc(S(C)(=O)=O)cc4)c(C#N)s3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL219711
Phase Preclinical
Structure Type MOL
InChI Key PZPCKANQRXHUSX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

469.5
MW (Da)
3.96
ALogP
9
HBA
0
HBD
103.4
PSA (Ų)
0.40
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19N3O5S2
MW 469.54
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase PLK1
CHEMBL3024
IC50 6.2 6.2 631.0 1
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 5.3 5.3 5011.9 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
16997559 10.1016/j.bmcl.2006.09.018 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
16997559 10.1016/j.bmcl.2006.09.018 Serine/threonine-protein kinase PLK1 1

Data from ChEMBL 36 via Core Engine