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Compound Detail

CHEMBL252455

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CSc1ncc2cc(-c3ccccc3)c(-c3ccc(CNCCc4nnc(N)s4)cc3)nc2n1

Basic Information

ChEMBL ID CHEMBL252455
Phase Preclinical
Structure Type MOL
InChI Key ZFGVHTJRILVQEN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
4.85
ALogP
9
HBA
2
HBD
102.5
PSA (Ų)
0.18
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N7S2
MW 485.64
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.36

Activity Summary

IC50 2 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 7.34 7.34 46.0 1
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 6.28 6.28 529.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 46.0 nM 7.34 Inhibition of Akt1 18249537
RAC-beta serine/threonine-protein kinase IC50 = 529.0 nM 6.28 Inhibition of Akt2 18249537

Literature References

PubMed DOI Target Context # Activities
18249537 10.1016/j.bmcl.2008.01.054 RAC-alpha serine/threonine-protein kinase 1
18249537 10.1016/j.bmcl.2008.01.054 RAC-beta serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine