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Compound Detail

CHEMBL429703

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c1ccc(-c2cc(C3CCN(Cc4ccc(-c5nc6ncccc6cc5-c5ccccc5)cc4)CC3)n[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL429703
Phase Preclinical
Structure Type MOL
InChI Key PTXPTLPZSUXRMX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

521.7
MW (Da)
7.73
ALogP
4
HBA
1
HBD
57.7
PSA (Ų)
0.24
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H31N5
MW 521.67
Aromatic Rings 6
Heavy Atoms 40
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.33 6.33 470.0 1
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 470.0 nM 6.33 Inhibition of Akt1 18479914
RAC-beta serine/threonine-protein kinase IC50 = 1600.0 nM 5.8 Inhibition of Akt2 18479914

Literature References

PubMed DOI Target Context # Activities
18479914 10.1016/j.bmcl.2008.04.074 Unchecked 3
18479914 10.1016/j.bmcl.2008.04.074 RAC-alpha serine/threonine-protein kinase 2
18479914 10.1016/j.bmcl.2008.04.074 RAC-beta serine/threonine-protein kinase 2

Data from ChEMBL 36 via Core Engine