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Compound Detail

CHEMBL378977

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O=S1(=O)Nc2ccc(N[C@H](COc3cncc(-c4ccc5c(c4)NS(=O)(=O)N5)c3)Cc3c[nH]c4ccccc34)cc2N1

Basic Information

ChEMBL ID CHEMBL378977
Phase Preclinical
Structure Type MOL
InChI Key VNLLALPIZGAWOM-NRFANRHFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

603.7
MW (Da)
4.50
ALogP
7
HBA
6
HBD
166.3
PSA (Ų)
0.15
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25N7O5S2
MW 603.69
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -0.54

Activity Summary

IC50 1 meas. best 4.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 4.81 4.81 15600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 15600.0 nM 4.81 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