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Compound Detail

CHEMBL471511

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O=C(Cc1ncc(CCNc2ncnc3ccsc23)s1)Nc1cccc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL471511
Phase Preclinical
Structure Type MOL
InChI Key USSPDYYDWFNICI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

463.5
MW (Da)
5.00
ALogP
7
HBA
2
HBD
79.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16F3N5OS2
MW 463.51
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -2.39

Activity Summary

IC50 2 meas. best 6.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
IC50 6.36 6.36 442.0 1
Aurora kinase A
CHEMBL4722
IC50 5.31 5.31 4900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase B IC50 = 442.0 nM 6.36 Inhibition of Aurora B by radiometric assay 18678489
Aurora kinase A IC50 = 4900.0 nM 5.31 Inhibition of Aurora A by radiometric assay 18678489

Literature References

PubMed DOI Target Context # Activities
18678489 10.1016/j.bmcl.2008.07.073 HCT-116 2
18678489 10.1016/j.bmcl.2008.07.073 Aurora kinase A 1
18678489 10.1016/j.bmcl.2008.07.073 Aurora kinase B 1

Data from ChEMBL 36 via Core Engine