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Compound Detail

CHEMBL4078832

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CCCCOC1CCc2nc3cc(Cl)ccc3c(NCCCCCCCCCNc3c4c(nc5cc(Cl)ccc35)CCC(OCCCC)C4)c2C1

Basic Information

ChEMBL ID CHEMBL4078832
Phase Preclinical
Structure Type MOL
InChI Key LWMHETDODOVEBY-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

733.9
MW (Da)
11.69
ALogP
6
HBA
2
HBD
68.3
PSA (Ų)
0.09
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H58Cl2N4O2
MW 733.87
Aromatic Rings 4
Heavy Atoms 51
NP-Likeness -0.21

Activity Summary

IC50 3 meas. best 6.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 6.38 6.375 420.0 2
J774.1
CHEMBL4296442
IC50 5.07 5.07 8600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28698054 10.1016/j.bmc.2017.06.051 Trypanosoma brucei brucei 2
28698054 10.1016/j.bmc.2017.06.051 Rhodesain 2
28698054 10.1016/j.bmc.2017.06.051 J774.1 1
28698054 10.1016/j.bmc.2017.06.051 Unchecked 1
28698054 10.1016/j.bmc.2017.06.051 Trypanothione reductase 1
28698054 10.1016/j.bmc.2017.06.051 Leishmania infantum 1

Data from ChEMBL 36 via Core Engine