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Compound Detail

CHEMBL596755

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COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1S(=O)(=O)CCCCCCC(=O)NO

Basic Information

ChEMBL ID CHEMBL596755
Phase Preclinical
Structure Type MOL
InChI Key FMDQBAXOPXWFEH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

511.0
MW (Da)
4.40
ALogP
8
HBA
3
HBD
130.5
PSA (Ų)
0.20
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24ClFN4O5S
MW 510.98
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.39

Activity Summary

IC50 2 meas. best 7.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.81 7.81 15.4 1
Histone deacetylase
CHEMBL2093865
IC50 6.92 6.92 121.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 15.4 nM 7.81 Inhibition of EGFR 20143778
Histone deacetylase IC50 = 121.7 nM 6.92 Inhibition of HDAC in human HeLa cell nuclear extract 20143778

Literature References

PubMed DOI Target Context # Activities
20143778 10.1021/jm901453q Histone deacetylase 1
20143778 10.1021/jm901453q Epidermal growth factor receptor 1
20143778 10.1021/jm901453q Receptor tyrosine-protein kinase erbB-2 1

Data from ChEMBL 36 via Core Engine