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Compound Detail

CHEMBL206708

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N[C@H](COc1cncc(/C=C/c2ccnc(-n3ccc4ccccc43)c2)c1)Cc1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL206708
Phase Preclinical
Structure Type MOL
InChI Key HJGRQCRBHSDOIH-OGJPMFGRSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
6.02
ALogP
5
HBA
2
HBD
81.8
PSA (Ų)
0.28
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H27N5O
MW 485.59
Aromatic Rings 6
Heavy Atoms 37
NP-Likeness -0.74

Activity Summary

IC50 2 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 5.48 5.48 3340.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 3340.0 nM 5.48 Inhibition of Akt1 using 10 uM ATP 16403626
RAC-alpha serine/threonine-protein kinase IC50 = 3340.0 nM 5.48 Inhibition of Akt 19497644

Literature References

PubMed DOI Target Context # Activities
16403626 10.1016/j.bmcl.2005.12.017 RAC-alpha serine/threonine-protein kinase 1
19497644 10.1016/j.ejmech.2009.04.050 RAC-alpha serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine