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Compound Detail

CHEMBL1084889

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Cn1ccnc1CN1CCN(c2c(Br)cnc3[nH]c(-c4ccc(CN5CCOCC5)cc4)nc23)CC1

Basic Information

ChEMBL ID CHEMBL1084889
Phase Preclinical
Structure Type MOL
InChI Key CMBJRFZUXFLZFO-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

551.5
MW (Da)
3.28
ALogP
8
HBA
1
HBD
78.3
PSA (Ų)
0.39
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H31BrN8O
MW 551.49
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.55

Activity Summary

IC50 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 7.52 7.52 30.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 30.0 nM 7.52 Inhibition of human recombinant Aurora A expressed in baculovirus system 20565112
Aurora kinase A IC50 = 30.0 nM 7.52 Inhibition of Aurora A 21093113

Literature References

PubMed DOI Target Context # Activities
20565112 10.1021/jm100262j Aurora kinase A 1
20565112 10.1021/jm100262j HCT-116 1
21093113 10.1016/j.ejmech.2010.10.017 Aurora kinase A 1

Data from ChEMBL 36 via Core Engine