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Compound Detail

CHEMBL4129991

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Cc1ccc(-c2ccccc2)cc1Nc1nccc(-c2ccc(C(N)=O)cc2)n1

Basic Information

ChEMBL ID CHEMBL4129991
Phase Preclinical
Structure Type MOL
InChI Key UTVHBHGNARQRMH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

380.4
MW (Da)
4.96
ALogP
4
HBA
2
HBD
80.9
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 C24H20N4O
MW 380.45
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.24

Activity Summary

IC50 2 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcium/calmodulin-dependent protein kinase kinase 2
CHEMBL5284
IC50 6.3 6.3 501.2 1
Calcium/calmodulin-dependent protein kinase kinase 2
CHEMBL4295888
IC50 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29653895 10.1016/j.bmcl.2018.03.034 Calcium/calmodulin-dependent protein kinase kinase 2 2
29653895 10.1016/j.bmcl.2018.03.034 No relevant target 1
29653895 10.1016/j.bmcl.2018.03.034 Glycogen synthase kinase-3 beta 1
29653895 10.1016/j.bmcl.2018.03.034 Mitogen-activated protein kinase 8 1
29653895 10.1016/j.bmcl.2018.03.034 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1

Data from ChEMBL 36 via Core Engine