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Compound Detail

CHEMBL1186058

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COc1cc2c(cc1OC)C(=O)C(CC1CCN(CCNc3c4c(nc5cc(Cl)ccc35)CCCC4)CC1)C2

Basic Information

ChEMBL ID CHEMBL1186058
Phase Preclinical
Structure Type MOL
InChI Key FNBJPXIAYRUTAU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

548.1
MW (Da)
6.35
ALogP
6
HBA
1
HBD
63.7
PSA (Ų)
0.35
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H38ClN3O3
MW 548.13
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.53

Activity Summary

IC50 2 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
IC50 6.52 6.52 300.0 1
Plasmodium falciparum
CHEMBL364
IC50 5.31 5.31 4860.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25678015 10.1016/j.bmc.2015.01.031 Trypanosoma brucei 2
25678015 10.1016/j.bmc.2015.01.031 Unchecked 2
25678015 10.1016/j.bmc.2015.01.031 Plasmodium falciparum 1
25678015 10.1016/j.bmc.2015.01.031 L6 1

Data from ChEMBL 36 via Core Engine