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Compound Detail

CHEMBL5396341

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CS(=O)(=O)O.CS(=O)(=O)O.c1cc2nc(CCCCc3nc4ccc(C5=NCCCN5)cc4s3)sc2cc1C1=NCCCN1

Basic Information

ChEMBL ID CHEMBL5396341
Phase Preclinical
Structure Type MOL
InChI Key MGYZDMQDZPCIQI-UHFFFAOYSA-N
Parent Compound CHEMBL5498607
Active Moiety CHEMBL5498607
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

488.7
MW (Da)
4.95
ALogP
8
HBA
2
HBD
74.6
PSA (Ų)
0.36
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36N6O6S4
MW 680.90
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.78

Activity Summary

EC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei
CHEMBL612849
EC50 6.72 6.72 190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei EC50 = 190.0 nM 6.72 Antitrypanosomal activity against blood stream form of Trypanosoma brucei 221a v... 37722077

Literature References

PubMed DOI Target Context # Activities
37722077 10.1021/acs.jmedchem.3c01051 Trypanosoma brucei 2
37722077 10.1021/acs.jmedchem.3c01051 L6 1
37722077 10.1021/acs.jmedchem.3c01051 ADMET 1

Data from ChEMBL 36 via Core Engine