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Compound Detail

CHEMBL4126300

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COc1ccccc1Nc1nccc(-c2ccc(C(=O)O)cc2)n1

Basic Information

ChEMBL ID CHEMBL4126300
Phase Preclinical
Structure Type MOL
InChI Key RGAZYDIYLXPGEV-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

321.3
MW (Da)
3.59
ALogP
5
HBA
2
HBD
84.3
PSA (Ų)
0.75
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 C18H15N3O3
MW 321.34
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.00

Activity Summary

IC50 3 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcium/calmodulin-dependent protein kinase kinase 2
CHEMBL5284
IC50 5.8 5.8 1584.9 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
IC50 5.4 5.4 3981.1 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.3 5.3 5011.9 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