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Compound Detail

CHEMBL377687

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O=C1Nc2ccc(N[C@H](COc3cncc(-c4ccc5c(c4)C(=O)C(=O)N5)c3)Cc3c[nH]c4ccccc34)cc2C1=O

Basic Information

ChEMBL ID CHEMBL377687
Phase Preclinical
Structure Type MOL
InChI Key BJBYRXGOEDKOAM-NRFANRHFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

557.6
MW (Da)
4.60
ALogP
7
HBA
4
HBD
142.3
PSA (Ų)
0.20
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 C32H23N5O5
MW 557.57
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -0.38

Activity Summary

IC50 1 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.75 6.75 179.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 179.0 nM 6.75 Inhibition of AKT1 in presence of 5 uM ATP 16644221

Literature References

PubMed DOI Target Context # Activities
16644221 10.1016/j.bmcl.2006.04.005 F5.12 1
16644221 10.1016/j.bmcl.2006.04.005 RAC-alpha serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine