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Compound Detail

CHEMBL587208

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OCCn1c(CNCCCNc2nc3ccccc3[nH]2)cc2c(Cl)cc(Cl)cc21

Basic Information

ChEMBL ID CHEMBL587208
Phase Preclinical
Structure Type MOL
InChI Key JCEOIIIPEPYSSD-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

432.4
MW (Da)
4.41
ALogP
5
HBA
4
HBD
77.9
PSA (Ų)
0.30
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23Cl2N5O
MW 432.36
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.19

Activity Summary

IC50 4 meas. best 9.0
EC50 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
IC50 9.0 9.0 1.0 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 6.16 6.16 691.8 1
Hexose transporter 1
CHEMBL4697
IC50 5.53 5.53 2935.0 1
Glucose transporter
CHEMBL3431938
IC50 5.51 5.51 3073.0 1
Solute carrier family 2, facilitated glucose transporter member 1
CHEMBL2535
IC50 5.25 5.25 5645.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 2
- 10.6019/CHEMBL3433997 Hexose transporter 1 2
- 10.6019/CHEMBL3433997 Glucose transporter 2
28189084 10.1016/j.ejmech.2017.01.040 Trypanosoma brucei brucei 2
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 1
28189084 10.1016/j.ejmech.2017.01.040 HepG2 1
28886510 10.1016/j.ejmech.2017.08.014 Unchecked 1
28886510 10.1016/j.ejmech.2017.08.014 Trypanosoma brucei 1

Data from ChEMBL 36 via Core Engine