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Compound Detail

CHEMBL3799807

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COc1nc(NCCc2c[nH]c3ccccc23)nc(Nc2ccc3[nH]ncc3c2)n1

Basic Information

ChEMBL ID CHEMBL3799807
Phase Preclinical
Structure Type MOL
InChI Key NSJQROISOSHTBB-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
3.64
ALogP
7
HBA
4
HBD
116.4
PSA (Ų)
0.33
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 C21H20N8O
MW 400.45
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.42

Activity Summary

IC50 4 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase PAK 4
CHEMBL4482
IC50 6.1 6.1 790.0 4

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27117431 10.1016/j.bmcl.2016.04.037 Serine/threonine-protein kinase PAK 4 1
28284095 10.1016/j.ejmech.2017.02.063 Serine/threonine-protein kinase PAK 4 1
29046238 10.1016/j.ejmech.2017.09.035 Serine/threonine-protein kinase PAK 4 1
35272236 10.1016/j.bmc.2022.116700 Serine/threonine-protein kinase PAK 4 1
25415869 10.1021/jm501613q Serine/threonine-protein kinase PAK 4 1

Data from ChEMBL 36 via Core Engine