Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL1872842

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
O=C(NCCc1csc(-c2ccccc2)n1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL1872842
Phase Preclinical
Structure Type MOL
InChI Key ZCTSQCRTBXPIIU-UHFFFAOYSA-N
8
Targets
21
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

308.4
MW (Da)
3.78
ALogP
3
HBA
1
HBD
42.0
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16N2OS
MW 308.41
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.74

Activity Summary

IC50 20 meas. best 7.11
EC50 1 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 7.11 7.11 78.0 1
Trypanosoma brucei
CHEMBL612849
IC50 6.82 6.81 150.0 2
Trypanosoma brucei brucei
CHEMBL612851
IC50 6.82 6.665 150.0 6
Trypanosoma cruzi
CHEMBL368
IC50 6.4 6.275 398.1 6
Trypanosoma brucei brucei
CHEMBL612851
EC50 6.26 6.26 550.0 1
Leishmania donovani
CHEMBL367
IC50 4.8 4.7 15848.9 2
NIH3T3
CHEMBL614822
IC50 4.7 4.7 19952.6 1
Plasmodium falciparum
CHEMBL364
IC50 4.5 4.5 32000.0 1
L6
CHEMBL614793
IC50 4.17 4.17 68000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma brucei rhodesiense IC50 = 78.0 nM 7.11 Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypoma... 27548560
Trypanosoma brucei IC50 = 150.0 nM 6.82 AntiTrypanosoma brucei activity T. b. brucei IC50 (uM) -
Trypanosoma brucei brucei IC50 = 150.0 nM 6.82 Antitrypanosomal activity against Trypanosoma brucei brucei by pathogen box scre... 30647879
Trypanosoma brucei IC50 = 160.0 nM 6.8 AntiTrypanosoma brucei activity T. b. rhodesiense IC50 (uM) -
Trypanosoma brucei brucei IC50 = 180.0 nM 6.75 Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream form... 30647879
Trypanosoma brucei brucei IC50 = 199.53 nM 6.7 GSK_TCAKS: pIC50 Trypanosoma brucei viability assay using fluorescence intensity... -
Trypanosoma brucei brucei IC50 = 240.0 nM 6.62 Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream form... 30647879
Trypanosoma brucei brucei IC50 = 250.0 nM 6.6 Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 strain bl... 27548560
Trypanosoma brucei brucei IC50 = 316.23 nM 6.5 GSK_TCAKS: pIC50 Trypanosoma brucei viability assay using luminiscence. Assay pl... -
Trypanosoma cruzi IC50 = 398.11 nM 6.4 GSK_TCAKS: pIC50 Trypanosoma cruzi Imaging: Amastigotes/Cell. H9c2 cells were se... -
Trypanosoma cruzi IC50 = 400.0 nM 6.4 Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain trypomastigo... 27548560
Trypanosoma cruzi IC50 = 501.19 nM 6.3 GSK_TCAKS: pIC50 Trypanosoma cruzi Imaging: Infected Cells. H9c2 cells were seed... -
Trypanosoma brucei brucei EC50 = 550.0 nM 6.26 Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei ... 27102161
Trypanosoma cruzi IC50 = 550.0 nM 6.26 Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 strain amastigot... 27548560
Trypanosoma cruzi IC50 = 562.34 nM 6.25 GSK_TCAKS: pIC50 Trypanosoma cruzi viability assay using beta-GAL activity. This... -
Trypanosoma cruzi IC50 = 920.0 nM 6.04 AntiTrypanosoma cruzi activity IC50 (uM) -
Leishmania donovani IC50 = 15848.93 nM 4.8 GSK_TCAKS: pIC50 Leishmania donovani Imaging: THP-1 Host Macrophages. Assay plat... -
NIH3T3 IC50 = 19952.62 nM 4.7 GSK_TCAKS: pIC50 NIH 3T3 cell line viability assay using luminiscence. Tissue cu... -
Leishmania donovani IC50 = 25000.0 nM 4.6 Antileishmanial activity against Leishmania donovani MHOM/ET/67/L82 amastigotes ... 27548560
Plasmodium falciparum IC50 = 32000.0 nM 4.5 Antiplasmodial activity against chloroquine and pyrimethamine resistant erythroc... 27548560

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3430912 Trypanosoma cruzi 4
- 10.6019/CHEMBL3430912 Leishmania donovani 4
30647879 10.1039/C8MD00319J Trypanosoma brucei brucei 4
27548560 10.1021/acs.jmedchem.6b00442 Trypanosoma cruzi 2
27548560 10.1021/acs.jmedchem.6b00442 Unchecked 2
- 10.6019/CHEMBL3832761 Trypanosoma brucei 2
- 10.6019/CHEMBL3430912 Trypanosoma brucei brucei 2
27102161 10.1016/j.bmc.2016.04.006 Trypanosoma brucei brucei 1
- 10.6019/CHEMBL3832761 MRC5 1
- 10.6019/CHEMBL3832761 NON-PROTEIN TARGET 1
- 10.6019/CHEMBL3832761 Trypanosoma cruzi 1
- 10.6019/CHEMBL3430912 Sterol 14-alpha demethylase 1
- 10.6019/CHEMBL3832761 Leishmania infantum 1
- 10.6019/CHEMBL3987221 Ferrochelatase, mitochondrial 1
- 10.6019/CHEMBL3987221 Porphobilinogen deaminase 1
- 10.6019/CHEMBL3430912 NIH3T3 1
30647879 10.1039/C8MD00319J HeLa 1
27548560 10.1021/acs.jmedchem.6b00442 Leishmania donovani 1
- 10.6019/CHEMBL4513149 Candida albicans 1
- 10.6019/CHEMBL4513149 Cryptococcus neoformans 1

Data from ChEMBL 36 via Core Engine