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Compound Detail

CHEMBL4867079

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O=C(Nc1cccc(Cl)c1)Nc1ncc(CCNc2ncnc3cc(F)ccc23)s1

Basic Information

ChEMBL ID CHEMBL4867079
Phase Preclinical
Structure Type MOL
InChI Key LPQVMJBOZXWART-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

442.9
MW (Da)
5.18
ALogP
6
HBA
3
HBD
91.8
PSA (Ų)
0.38
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16ClFN6OS
MW 442.91
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -2.36

Activity Summary

IC50 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase A
CHEMBL4722
IC50 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase A IC50 = 9.0 nM 8.05 Inhibition of recombinant GST-AURKA (residues Ser123 to Ser401) (unknown origin)... 34606263

Literature References

PubMed DOI Target Context # Activities
34606263 10.1021/acs.jmedchem.1c01006 Aurora kinase A 2
34606263 10.1021/acs.jmedchem.1c01006 Macrophage colony-stimulating factor 1 receptor 1
34606263 10.1021/acs.jmedchem.1c01006 Aurora kinase B 1

Data from ChEMBL 36 via Core Engine