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Compound Detail

CHEMBL4534157

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O=[N+]([O-])c1c(CS(=O)(=O)c2ccccc2)nc2c(Sc3ccc(Cl)cc3)cc(Cl)cn12

Basic Information

ChEMBL ID CHEMBL4534157
Phase Preclinical
Structure Type MOL
InChI Key GMELBBZUKRQOIY-UHFFFAOYSA-N
8
Targets
14
Activities
2
Assay Types
1
PK Parameters
17
Publications
0
Known Names

Molecular Properties

494.4
MW (Da)
5.67
ALogP
7
HBA
0
HBD
94.6
PSA (Ų)
0.25
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H13Cl2N3O4S2
MW 494.38
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.70

Activity Summary

IC50 12 meas. best 7.48
EC50 2 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.48 7.0 33.0 2
Leishmania donovani
CHEMBL367
IC50 6.58 6.1933 260.0 3
Leishmania donovani
CHEMBL367
EC50 6.0 6.0 1000.0 1
Trypanosoma brucei brucei
CHEMBL612851
EC50 5.89 5.89 1300.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 5.89 5.89 1300.0 1
Leishmania major
CHEMBL612879
IC50 5.89 5.785 1300.0 2
Leishmania infantum
CHEMBL612848
IC50 5.77 5.77 1700.0 1
Trypanosoma cruzi
CHEMBL368
IC50 5.66 5.66 2200.0 1
Trichomonas vaginalis
CHEMBL612884
IC50 5.34 5.34 4600.0 1
Plasmodium falciparum
CHEMBL364
IC50 4.72 4.72 19000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.05 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 33.0 nM 7.48 Substrate activity at NTR1 in promastigote stage of Leishmania donovani MHOM/SD/... 30655943
Leishmania donovani IC50 = 260.0 nM 6.58 Antileishmanial activity against wild type promastigote stage of Leishmania dono... 30655943
Unchecked IC50 = 300.0 nM 6.52 Substrate activity at NTR2 in promastigote stage of Leishmania donovani MHOM/SD/... 30655943
Leishmania donovani EC50 = 1000.0 nM 6.0 Antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigot... 32652409
Leishmania donovani IC50 = 1000.0 nM 6.0 Antileishmanial activity against promastigote stage of Leishmania donovani MHOM/... 30655943
Leishmania donovani IC50 = 1000.0 nM 6.0 Antileishmanial activity against intracellular amastigote stage of Leishmania do... 30655943
Trypanosoma brucei brucei EC50 = 1300.0 nM 5.89 Antileishmanial activity against Trypanosoma brucei brucei AnTat 1.9 measured af... 32652409
Leishmania major IC50 = 1300.0 nM 5.89 Antileishmanial activity against promastigote stage of Leishmania major MHOM/IL/... 30655943
Trypanosoma brucei brucei IC50 = 1300.0 nM 5.89 Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei bru... 30655943
Leishmania infantum IC50 = 1700.0 nM 5.77 Antileishmanial activity against Leishmania infantum axenic amastigotes after 48... 30655943
Leishmania major IC50 = 2100.0 nM 5.68 Antileishmanial activity against intracellular amastigote stage of Leishmania ma... 30655943
Trypanosoma cruzi IC50 = 2200.0 nM 5.66 Antitrypanosomal activity against Trypanosoma cruzi MHOM/BR/78/Silvio cloneX10/7... 30655943
Trichomonas vaginalis IC50 = 4600.0 nM 5.34 Antiprotozoal activity against Trichomonas vaginalis TVR87 measured after 48 hrs... 30655943
Plasmodium falciparum IC50 = 19000.0 nM 4.72 Antiplasmodial activity against chloroquine/proguanil/pyrimethamine-resistant sy... 30655943

Literature References

Data from ChEMBL 36 via Core Engine