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Compound Detail

CHEMBL560143

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CONC(=N)c1ccc(OCc2cccc(COc3ccc(C(=N)NOC)cc3)c2)cc1

Basic Information

ChEMBL ID CHEMBL560143
Phase Preclinical
Structure Type MOL
InChI Key BQKBZANMNZBQQS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
3.80
ALogP
6
HBA
4
HBD
108.7
PSA (Ų)
0.22
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26N4O4
MW 434.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.34

Activity Summary

IC50 1 meas. best 4.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 4.52 4.52 30400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei rhodesiense IC50 = 30400.0 nM 4.52 Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 19409677

Literature References

PubMed DOI Target Context # Activities
19409677 10.1016/j.ejmech.2009.03.014 Trypanosoma brucei rhodesiense 3
19409677 10.1016/j.ejmech.2009.03.014 Unchecked 3
19409677 10.1016/j.ejmech.2009.03.014 Plasmodium falciparum 1
19409677 10.1016/j.ejmech.2009.03.014 Leishmania donovani 1
19409677 10.1016/j.ejmech.2009.03.014 L6 1

Data from ChEMBL 36 via Core Engine