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Compound Detail

CHEMBL358287

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N=C(N)c1ccc(-c2ccc(-c3ccc(C(=N)N)cn3)o2)nc1

Basic Information

ChEMBL ID CHEMBL358287
Phase Preclinical
Structure Type MOL
InChI Key YIOIBLVIGXIOMG-UHFFFAOYSA-N
4
Targets
7
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

306.3
MW (Da)
1.97
ALogP
5
HBA
4
HBD
138.7
PSA (Ų)
0.43
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H14N6O
MW 306.33
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.48

Activity Summary

IC50 7 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 7.89 7.89 13.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 7.72 7.6933 19.0 3
Plasmodium falciparum
CHEMBL364
IC50 7.08 7.08 83.0 2
L6
CHEMBL614793
IC50 4.08 4.08 83000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19620327 10.1128/aac.00225-09 Trypanosoma brucei rhodesiense 9
19620327 10.1128/aac.00225-09 Trypanosoma brucei brucei 8
19620327 10.1128/aac.00225-09 Trypanosoma brucei gambiense 4
24012380 10.1016/j.bmc.2013.08.006 Trypanosoma brucei rhodesiense 4
17517831 10.1128/aac.00005-07 Unchecked 3
19620327 10.1128/aac.00225-09 Unchecked 3
14561095 10.1021/jm0302602 Nucleic Acid 2
14561095 10.1021/jm0302602 Mus musculus 2
14561095 10.1021/jm0302602 Trypanosoma brucei rhodesiense 1
14561095 10.1021/jm0302602 Plasmodium falciparum 1
17517831 10.1128/aac.00005-07 Trypanosoma brucei brucei 1
17517831 10.1128/aac.00005-07 Trypanosoma brucei rhodesiense 1
24012380 10.1016/j.bmc.2013.08.006 L6 1
24012380 10.1016/j.bmc.2013.08.006 Plasmodium falciparum 1
24012380 10.1016/j.bmc.2013.08.006 Unchecked 1

Data from ChEMBL 36 via Core Engine