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Compound Detail

CHEMBL2177124

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NCCCCNCc1ccc(OC2=CC(=O)c3cc4ccccc4cc3C2=O)cc1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL2177124
Phase Preclinical
Structure Type MOL
InChI Key RRKAFODIXVPONT-UHFFFAOYSA-N
Parent Compound CHEMBL2221052
Active Moiety CHEMBL2221052
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

400.5
MW (Da)
4.01
ALogP
5
HBA
2
HBD
81.4
PSA (Ų)
0.56
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25F3N2O5
MW 514.50
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness 0.34

Activity Summary

IC50 5 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 6.46 6.46 350.0 1
Leishmania donovani
CHEMBL367
IC50 5.55 5.5 2820.0 2
L6
CHEMBL614793
IC50 5.25 5.25 5600.0 1
Trypanosoma cruzi
CHEMBL368
IC50 4.73 4.73 18600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23153330 10.1021/jm301112z Unchecked 4
23153330 10.1021/jm301112z Trypanothione reductase 2
23153330 10.1021/jm301112z Leishmania donovani 2
23153330 10.1021/jm301112z L6 1
23153330 10.1021/jm301112z Trypanosoma cruzi 1
23153330 10.1021/jm301112z Trypanosoma brucei rhodesiense 1

Data from ChEMBL 36 via Core Engine