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Compound Detail

CHEMBL4632948

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CC(C)Oc1cc(N2CCC(O)CC2)ccc1Nc1ncc2c(n1)N(C)c1ccccc1C(=O)N2C

Basic Information

ChEMBL ID CHEMBL4632948
Phase Preclinical
Structure Type MOL
InChI Key NPRYKZQCTXZUKH-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

488.6
MW (Da)
4.33
ALogP
8
HBA
2
HBD
94.1
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N6O3
MW 488.59
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.02

Activity Summary

IC50 4 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leucine-rich repeat serine/threonine-protein kinase 2
CHEMBL1075104
IC50 6.8 6.695 160.0 2
Serine/threonine-protein kinase DCLK1
CHEMBL5683
IC50 6.29 6.29 510.0 1
Mitogen-activated protein kinase 7
CHEMBL5332
IC50 5.82 5.82 1530.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24239623 10.1016/j.ejmech.2013.10.052 Mitogen-activated protein kinase 7 2
32530623 10.1021/acs.jmedchem.0c00596 Serine/threonine-protein kinase DCLK1 1
32530623 10.1021/acs.jmedchem.0c00596 Mitogen-activated protein kinase 7 1
32530623 10.1021/acs.jmedchem.0c00596 Leucine-rich repeat serine/threonine-protein kinase 2 1
24239623 10.1016/j.ejmech.2013.10.052 Leucine-rich repeat serine/threonine-protein kinase 2 1

Data from ChEMBL 36 via Core Engine