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Compound Detail

CHEMBL58173

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c1cc(-c2ccc(-c3ccc(C4=NCCN4)cc3)o2)ccc1C1=NCCN1

Basic Information

ChEMBL ID CHEMBL58173
Phase Preclinical
Structure Type MOL
InChI Key VOFBXZAWHLGYKW-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

356.4
MW (Da)
3.31
ALogP
5
HBA
2
HBD
61.9
PSA (Ų)
0.75
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 C22H20N4O
MW 356.43
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.25

Activity Summary

IC50 3 meas. best 6.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 6.61 6.61 245.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 6.6 6.6 251.0 1
B16
CHEMBL381
IC50 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17517831 10.1128/aac.00005-07 Unchecked 3
11985467 10.1021/jm010539n B16 1
17517831 10.1128/aac.00005-07 Trypanosoma brucei rhodesiense 1
17517831 10.1128/aac.00005-07 Trypanosoma brucei brucei 1
20153561 10.1016/j.ejmech.2010.01.047 Nucleic Acid 1

Data from ChEMBL 36 via Core Engine