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Compound Detail

CHEMBL117064

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COc1cccc2c1cc1c3ccccc3nc-1n2C

Basic Information

ChEMBL ID CHEMBL117064
Phase Preclinical
Structure Type MOL
InChI Key FJJGFKBPRNRITA-UHFFFAOYSA-N
4
Targets
8
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

262.3
MW (Da)
3.84
ALogP
3
HBA
0
HBD
27.1
PSA (Ų)
0.52
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N2O
MW 262.31
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.52

Activity Summary

IC50 8 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
IC50 6.0 5.945 1000.0 2
Trypanosoma cruzi
CHEMBL368
IC50 5.4 5.4 4000.0 2
MRC5
CHEMBL614181
IC50 5.3 5.3 5000.0 1
Plasmodium falciparum
CHEMBL364
IC50 4.91 4.8033 12300.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12139461 10.1021/jm011102i Plasmodium falciparum 2
12139461 10.1021/jm011102i MRC5 1
12139461 10.1021/jm011102i Trypanosoma brucei 1
12139461 10.1021/jm011102i Trypanosoma cruzi 1
12139461 10.1021/jm011102i Nucleic Acid 1
12139461 10.1021/jm011102i Histidine-rich protein PFHRP-II 1
20185316 10.1016/j.bmc.2010.01.068 Plasmodium falciparum 1
20185316 10.1016/j.bmc.2010.01.068 Trypanosoma cruzi 1
20185316 10.1016/j.bmc.2010.01.068 Trypanosoma brucei 1

Data from ChEMBL 36 via Core Engine