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Compound Detail

CHEMBL268345

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COc1cc2c(Nc3cc(CC(=O)Nc4cccc([N+](=O)[O-])c4)[nH]n3)ncnc2cc1OCCCN1CCC(CO)CC1

Basic Information

ChEMBL ID CHEMBL268345
Phase Preclinical
Structure Type MOL
InChI Key PJXJTLKNCJRPQT-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

590.6
MW (Da)
3.67
ALogP
11
HBA
4
HBD
180.7
PSA (Ų)
0.10
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34N8O6
MW 590.64
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.40

Activity Summary

Ki 2 meas. best 7.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
Ki 7.41 6.73 39.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A Ki = 39.0 nM 7.41 Inhibition of human recombinant Aurora A 17373783
Aurora kinase A Ki = 890.0 nM 6.05 Inhibition of human recombinant Aurora A 17373783

Literature References

PubMed DOI Target Context # Activities
17373783 10.1021/jm061335f Aurora kinase A 2
17373783 10.1021/jm061335f SW-620 1

Data from ChEMBL 36 via Core Engine