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Compound Detail

CHEMBL3125730

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COc1ccc(-c2nc3cc(-c4csc(C(=O)NCC(C)(C)CO)c4)cnc3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL3125730
Phase Preclinical
Structure Type MOL
InChI Key SSAAGCQGRIMQSH-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
4.11
ALogP
6
HBA
3
HBD
100.1
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 C23H24N4O3S
MW 436.54
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.14

Activity Summary

IC50 4 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 7.0 6.935 100.0 2
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 6.48 6.48 330.0 1
Aurora kinase B
CHEMBL2185
IC50 5.78 5.78 1680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24462666 10.1016/j.bmcl.2013.12.123 Serine/threonine-protein kinase TBK1 2
24462666 10.1016/j.bmcl.2013.12.123 Cyclin-dependent kinase 2 1
24462666 10.1016/j.bmcl.2013.12.123 Aurora kinase B 1
24462666 10.1016/j.bmcl.2013.12.123 Inhibitor of nuclear factor kappa-B kinase subunit epsilon 1

Data from ChEMBL 36 via Core Engine