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Compound Detail

CHEMBL270847

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O=c1[nH]c2ccccc2n1C1CCN(Cc2ccc(-c3ncc(-c4nnn[nH]4)cc3-c3ccccc3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL270847
Phase Preclinical
Structure Type MOL
InChI Key INUGOQWCVGGZKS-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

528.6
MW (Da)
5.08
ALogP
7
HBA
2
HBD
108.4
PSA (Ų)
0.31
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H28N8O
MW 528.62
Aromatic Rings 6
Heavy Atoms 40
NP-Likeness -1.32

Activity Summary

IC50 2 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.8 6.8 157.0 1
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.56 6.56 273.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18294842 10.1016/j.bmcl.2007.12.040 RAC-alpha serine/threonine-protein kinase 2
18294842 10.1016/j.bmcl.2007.12.040 RAC-beta serine/threonine-protein kinase 2
15686884 10.1016/j.bmcl.2004.12.062 RAC-alpha serine/threonine-protein kinase 1
15686884 10.1016/j.bmcl.2004.12.062 Unchecked 1
15686884 10.1016/j.bmcl.2004.12.062 RAC-beta serine/threonine-protein kinase 1
18294842 10.1016/j.bmcl.2007.12.040 RAC-gamma serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine