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Compound Detail

CHEMBL552385

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Cc1cc(Nc2nc(Sc3ccc(Cl)c(Cl)c3)nc3ccccc23)n[nH]1

Basic Information

ChEMBL ID CHEMBL552385
Phase Preclinical
Structure Type MOL
InChI Key DXMLBGPNBMGQFP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

402.3
MW (Da)
5.86
ALogP
5
HBA
2
HBD
66.5
PSA (Ų)
0.42
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H13Cl2N5S
MW 402.31
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.80

Activity Summary

Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
Ki 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A Ki = 2.0 nM 8.7 Inhibition of Aurora-A by coupled assay 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