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Compound Detail

CHEMBL4063546

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C1=Cc2c(nc3ccccc3c2NCCCCCCNc2c3c(nc4ccccc24)CCC=C3)CC1

Basic Information

ChEMBL ID CHEMBL4063546
Phase Preclinical
Structure Type MOL
InChI Key DNBABFLPDWBYIL-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

474.6
MW (Da)
7.79
ALogP
4
HBA
2
HBD
49.8
PSA (Ų)
0.24
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34N4
MW 474.65
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.01

Activity Summary

IC50 3 meas. best 6.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 6.29 6.225 510.0 2
J774.1
CHEMBL4296442
IC50 5.75 5.75 1800.0 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 J774.1 1
28698054 10.1016/j.bmc.2017.06.051 Unchecked 1
28698054 10.1016/j.bmc.2017.06.051 No relevant target 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