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Compound Detail

CHEMBL1085134

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CN(C)c1ccc(-c2nc3c(N4CCN(S(=O)(=O)c5ccccc5)CC4)c(Br)cnc3[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL1085134
Phase Preclinical
Structure Type MOL
InChI Key LLNXIEBQULOTRS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

541.5
MW (Da)
3.96
ALogP
6
HBA
1
HBD
85.4
PSA (Ų)
0.41
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25BrN6O2S
MW 541.48
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.58

Activity Summary

IC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 6.75 6.75 178.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 178.0 nM 6.75 Inhibition of human recombinant Aurora A expressed in baculovirus system 20565112
Aurora kinase A IC50 = 178.0 nM 6.75 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