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Compound Detail

CHEMBL551634

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COc1ccccc1Sc1nc(Nc2cc(C)[nH]n2)c2ccccc2n1

Basic Information

ChEMBL ID CHEMBL551634
Phase Preclinical
Structure Type MOL
InChI Key CWQTZVUENDFTLF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
4.56
ALogP
6
HBA
2
HBD
75.7
PSA (Ų)
0.51
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H17N5OS
MW 363.45
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.45

Activity Summary

Ki 3 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
Ki 7.62 7.62 24.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 6.67 6.67 216.0 1
Aurora kinase B
CHEMBL2185
Ki 6.0 6.0 995.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A Ki = 24.0 nM 7.62 Inhibition of Aurora-A by coupled assay 19447622
Glycogen synthase kinase-3 beta Ki = 216.0 nM 6.67 Inhibition of GSK3-beta 19447622
Aurora kinase B Ki = 995.0 nM 6.0 Inhibition of Aurora-B 19447622

Literature References

PubMed DOI Target Context # Activities
19447622 10.1016/j.bmcl.2009.04.136 Aurora kinase A 1
19447622 10.1016/j.bmcl.2009.04.136 Aurora kinase B 1
19447622 10.1016/j.bmcl.2009.04.136 Proto-oncogene tyrosine-protein kinase Src 1
19447622 10.1016/j.bmcl.2009.04.136 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine