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Compound Detail

CHEMBL219899

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

Basic Information

ChEMBL ID CHEMBL219899
Phase Preclinical
Structure Type MOL
InChI Key YYZTVTZCYVZGRB-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
3.19
ALogP
9
HBA
1
HBD
122.7
PSA (Ų)
0.40
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21N3O6S2
MW 487.56
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.04

Activity Summary

IC50 2 meas. best 7.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase PLK1
CHEMBL3024
IC50 7.12 7.01 75.0 2

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
19097784 10.1016/j.bmcl.2008.11.041 Serine/threonine-protein kinase PLK1 1
19097784 10.1016/j.bmcl.2008.11.041 HCT-116 1

Data from ChEMBL 36 via Core Engine