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Compound Detail

CHEMBL3143722

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O=c1[nH]c(-c2ccc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2)c(-c2ccccc2)nc1Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL3143722
Phase Preclinical
Structure Type MOL
InChI Key QLBBPXPJCASIMV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

567.7
MW (Da)
6.17
ALogP
5
HBA
2
HBD
86.8
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 C36H33N5O2
MW 567.69
Aromatic Rings 6
Heavy Atoms 43
NP-Likeness -0.92

Activity Summary

IC50 2 meas. best 5.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-beta serine/threonine-protein kinase
CHEMBL2431
IC50 5.76 5.76 1755.0 1
RAC-gamma serine/threonine-protein kinase
CHEMBL4816
IC50 5.4 5.4 3973.0 1

Activity Data Samples

Top measurements by pChEMBL value

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