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Compound Detail

CHEMBL203945

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COc1cc2c(Nc3cnc(NC(=O)c4cccc(Cl)c4)nc3)ncnc2cc1OCCCN1CCCCC1

Basic Information

ChEMBL ID CHEMBL203945
Phase Preclinical
Structure Type MOL
InChI Key VORYRVZJHGILPD-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

548.0
MW (Da)
5.33
ALogP
9
HBA
2
HBD
114.4
PSA (Ų)
0.25
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30ClN7O3
MW 548.05
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.45

Activity Summary

IC50 3 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 9.1 9.1 0.8 2
MCF7
CHEMBL387
IC50 7.62 7.62 24.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 0.8 nM 9.1 Inhibitory activity against Aurora A 16337122
Aurora kinase A IC50 = 0.8 nM 9.1 Inhibition of Aurora A 16884290
MCF7 IC50 = 24.0 nM 7.62 Antiproliferative activity against MCF7 cell line 16337122

Literature References

PubMed DOI Target Context # Activities
16337122 10.1016/j.bmcl.2005.11.053 No relevant target 1
16337122 10.1016/j.bmcl.2005.11.053 Aurora kinase A 1
16337122 10.1016/j.bmcl.2005.11.053 MCF7 1
16884290 10.1021/jm060522a Aurora kinase A 1

Data from ChEMBL 36 via Core Engine