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Compound Detail

CHEMBL548436

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Cl.N=C(N)Nc1ccc(NC(=O)Nc2ccc(NC(=N)N)cc2)cc1

Basic Information

ChEMBL ID CHEMBL548436
Phase Preclinical
Structure Type MOL
InChI Key UFAIBRQWVORPLQ-UHFFFAOYSA-N
Parent Compound CHEMBL528397
Active Moiety CHEMBL528397
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

326.4
MW (Da)
1.94
ALogP
3
HBA
8
HBD
164.9
PSA (Ų)
0.32
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H19ClN8O
MW 362.82
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.53

Activity Summary

IC50 2 meas. best 7.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 7.02 7.02 96.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 6.73 6.73 187.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
18247550 10.1021/jm7013088 Unchecked 3
18247550 10.1021/jm7013088 Trypanosoma brucei rhodesiense 1
18247550 10.1021/jm7013088 Plasmodium falciparum 1
18247550 10.1021/jm7013088 L6 1
18247550 10.1021/jm7013088 Mus musculus 1
18247550 10.1021/jm7013088 Ferriprotoporphyrin IX 1
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1

Data from ChEMBL 36 via Core Engine