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Compound Detail

CHEMBL428861

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CCC(C)c1nc(-c2ccc(CN3CCC(n4c(O)nc5ccccc54)CC3)cc2)c(-c2ccccc2)nc1O

Basic Information

ChEMBL ID CHEMBL428861
Phase Preclinical
Structure Type MOL
InChI Key ILSSGVAAXSWLME-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

533.7
MW (Da)
6.92
ALogP
7
HBA
2
HBD
87.3
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H35N5O2
MW 533.68
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -0.80

Activity Summary

IC50 1 meas. best 4.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 4.77 4.77 17000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 17000.0 nM 4.77 Inhibitory concentration against human Protein kinase B, alpha 15664853

Literature References

PubMed DOI Target Context # Activities
15664853 10.1016/j.bmcl.2004.11.011 RAC-alpha serine/threonine-protein kinase 1
15664853 10.1016/j.bmcl.2004.11.011 RAC-beta serine/threonine-protein kinase 1
15664853 10.1016/j.bmcl.2004.11.011 RAC-gamma serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine