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Compound Detail

CHEMBL520654

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COc1cc(C2=NCCN2)cc2cc(-c3ccc(C4=NCCN4)cc3)oc12

Basic Information

ChEMBL ID CHEMBL520654
Phase Preclinical
Structure Type MOL
InChI Key SCGRUHAJSQVIGC-UHFFFAOYSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

360.4
MW (Da)
2.81
ALogP
6
HBA
2
HBD
71.2
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 C21H20N4O2
MW 360.42
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness 0.14

Activity Summary

IC50 7 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 7.5 7.5 32.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 6.91 6.91 124.0 1
Trypanosoma brucei
CHEMBL612849
IC50 6.11 5.475 780.0 2
Leishmania donovani
CHEMBL367
IC50 5.35 5.35 4500.0 1
Trypanosoma cruzi
CHEMBL368
IC50 4.88 4.88 13330.0 1
L6
CHEMBL614793
IC50 4.7 4.7 19900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18841956 10.1021/jm800918v Trypanosoma brucei rhodesiense 3
18841956 10.1021/jm800918v Unchecked 3
- 10.6019/CHEMBL3832761 Trypanosoma brucei 2
- 10.6019/CHEMBL4513149 HEK293 1
18841956 10.1021/jm800918v L6 1
- 10.6019/CHEMBL4513149 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513149 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4513149 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513149 Escherichia coli 1
- 10.6019/CHEMBL4513149 Cryptococcus neoformans 1
- 10.6019/CHEMBL4513149 Candida albicans 1
- 10.6019/CHEMBL4513101 Naegleria gruberi 1
- 10.6019/CHEMBL3987221 Porphobilinogen deaminase 1
- 10.6019/CHEMBL3987221 Ferrochelatase, mitochondrial 1
- 10.6019/CHEMBL3832761 HepG2 1
- 10.6019/CHEMBL3832761 Leishmania infantum 1
- 10.6019/CHEMBL3832761 Trypanosoma cruzi 1
- 10.6019/CHEMBL3832761 NON-PROTEIN TARGET 1
- 10.6019/CHEMBL3832761 MRC5 1
18841956 10.1021/jm800918v Leishmania donovani 1

Data from ChEMBL 36 via Core Engine