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Compound Detail

CHEMBL2312142

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COc1cc(Nc2cc(-c3cccc(C#N)c3)ccn2)ccc1N1CCN(C)CC1

Basic Information

ChEMBL ID CHEMBL2312142
Phase Preclinical
Structure Type MOL
InChI Key YTRKGSFSZXFLJT-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
4.12
ALogP
6
HBA
1
HBD
64.4
PSA (Ų)
0.70
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 C24H25N5O
MW 399.50
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.47

Activity Summary

IC50 3 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TRAF2 and NCK-interacting protein kinase
CHEMBL4527
IC50 8.22 6.395 6.0 2
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23232060 10.1016/j.bmcl.2012.11.013 TRAF2 and NCK-interacting protein kinase 4
23232060 10.1016/j.bmcl.2012.11.013 Caco-2 3
23232060 10.1016/j.bmcl.2012.11.013 Serine/threonine-protein kinase Chk1 1
23232060 10.1016/j.bmcl.2012.11.013 CDK6/cyclin D1 1
23232060 10.1016/j.bmcl.2012.11.013 Macrophage colony-stimulating factor 1 receptor 1
23232060 10.1016/j.bmcl.2012.11.013 Mitogen-activated protein kinase kinase kinase kinase 4 1
23232060 10.1016/j.bmcl.2012.11.013 Inhibitor of nuclear factor kappa-B kinase subunit epsilon 1
23232060 10.1016/j.bmcl.2012.11.013 Receptor-type tyrosine-protein kinase FLT3 1
23232060 10.1016/j.bmcl.2012.11.013 Voltage-gated inwardly rectifying potassium channel KCNH2 1
23232060 10.1016/j.bmcl.2012.11.013 No relevant target 1

Data from ChEMBL 36 via Core Engine