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Compound Detail

CHEMBL542698

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CNc1nc(NC)nc(NCCCNCCCCCCCCCCCCNCCCNc2nc(NC)nc(NC)n2)n1.Cl

Basic Information

ChEMBL ID CHEMBL542698
Phase Preclinical
Structure Type MOL
InChI Key KPUUGPJTBSMYJE-UHFFFAOYSA-N
Parent Compound CHEMBL1191581
Active Moiety CHEMBL1191581
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

588.9
MW (Da)
3.61
ALogP
14
HBA
8
HBD
173.6
PSA (Ų)
0.07
QED
3
Ro5 Violations
27
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H57ClN14
MW 625.31
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness -0.25

Activity Summary

IC50 4 meas. best 5.64
Ki 1 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 5.64 5.64 2300.0 1
Adenosine transporter 1
CHEMBL2601
Ki 5.5 5.5 3200.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 4.77 4.77 17000.0 1
ADMET
CHEMBL612558
IC50 4.75 4.75 18000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11585449 10.1021/jm010854+ Adenosine transporter 1 1
11585449 10.1021/jm010854+ Trypanosoma brucei rhodesiense 1
11585449 10.1021/jm010854+ Trypanosoma brucei brucei 1
11585449 10.1021/jm010854+ ADMET 1
11585449 10.1021/jm010854+ Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine